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The importance of essential metal ions and their metal complexes in the creation of prospective medical therapies has long been recognized. In chemistry, molecular biology, and medicinal fields; the interaction of metal complexes with DNA has been a subject of study. The dithiocarbamate essential metal complex is described extensively in the literature for its various benefits and advantages. With proper use of ligands, it is proven to increase the cytotoxic activity of metal complexes against cancer cells. Some researches have shown significant progress regarding the biological activities of the dithiocarbamate essential metal complex as antimicrobial, antioxidant, and anticancer agents. Metal complexes form complexes with dithiocarbamate ligands with unique structural variations. In this study, we presented an overview of the cytotoxic effects of some dithiocarbamate essential metal complexes on cancer cells, as well as fresh approaches to the design of essential metal-based therapeutics containing dithiocarbamate and molecular targets in cancer therapy. This review may provide an update on recent developments in the medicinal use of essential metals with dithiocarbamate ligands, carried out to identify recent relevant literature. Finally, we predict that the essential metal complexed with dithiocarbamate can be a new breakthrough in the future development of cancer drugs.

Efficient and mild synthetic routes for bioactive natural product derivatives are of current interest for drug discovery. Herein, on the basis of the pharmacophore hybrid strategy, we report a two-step protocol to obtain a series of structurally novel oleanolic acid (OA)-dithiocarbamate conjugates in mild conditions with high yields. Moreover, biological evaluations indicated that representative compound 3e exhibited the most potent and broad-spectrum antiproliferative effects against Panc1, A549, Hep3B, Huh-7, HT-29, and Hela cells with low cytotoxicity on normal cells. In terms of the IC50 values, these OA-dithiocarbamate conjugates were up to 30-fold more potent than the natural product OA. These compounds may be promising hit compounds for the development of novel anti-cancer drugs. [ABSTRACT FROM AUTHOR]

The uncontrolled concentrations of heavy metals introduced into the water sources need an effective method for their removal. The dithiocarbamate (dtc) ligands are the most popular precipitating agents used for the removal of metals from wastewater. Presently, two novel dtc ligands, one without methylene linker (K2L1) and the other with methylene linker (K2L2) were used for the removal of eight heavy metals ions including Fe2+, Co2+, Ni2+, Cu2+, Cd2+, Ag+, Zn2+ and Pb2+ from the aqueous solution. These dtc ligands contain acyl (NH-C = O) and S, S (thiolate) functional groups. The results indicated that the metal removal efficiency of both ligands was almost 100% at pH 4 and 7 and free of the linker effect and acyl functional groups but depends on the S, S binding sites. It exhibited a distinct selectivity for the removal of metal ions (Pb2+ ∼ Cu2+ ∼ Ag1+ > Cd2+ > Co2+ > Ni2+ > Zn2+ > Fe2+). The developed methods have the potential for the removal of heavy metals and can be used for other thiophilic metals that are water-soluble. HIGHLIGHTS Water treatment, contaminated by heavy metal ions. Synthesis and characterization of two novel dithiocarbamate ligands. Effect of methylene (-CH2-) linker of dithiocarbamtes on heavy metals extraction. pH and temperature effect on the extraction efficiency of ligands. [ABSTRACT FROM AUTHOR]

Human DNA ligase I (hLigI) plays an important role in the process of DNA replication and repair mechanisms, making it an important target for cancer. This article reports the design, synthesis, and biological activity of a series of 59 curcumin-monocarbonyl-dithiocarbamate hybrid molecules. Many of the synthetic compounds tested in this study showed a significant inhibitory effect on hLig1 activity (>90% inhibition) and demonstrated significant antiproliferative activity against colon cancer cells (DLD-1) at the 10 µM concentrations, with certain compounds showing selective activity against DLD-1 as compared to the normal HEK-293 and VERO cell line. The activity of curcuminoids were compared against Doxorubicin and Bleomycin which were used as positive control compounds with activity towards hLigI. Further, we checked the cytotoxicity of two compounds (27 and 49) along with positive control Doxorubicin in a concentration-dependent manner against DLD-1, HEK293, and VERO cell lines. Overall, our studies demonstrated that compounds 27 and 49 have significantly better hLigI inhibition and targeted cytotoxic activities than the previously reported monocarbonyl-curcumin hybrid compound 23*. This study brings us a step closer towards our quest to explore the molecular space for novel hLig1 inhibitors that will be suitable for clinical trials in cancer patients. [ABSTRACT FROM AUTHOR]

An approach to synthesize α‐substituted alkene derivatives via calcium‐promoted hydrothiolation of allenoates is described. Employing diverse allenoates, and amines, a library of α‐substituted alkenes is obtained with great regioselectivity and good to high yields. The reaction proceeds through the nucleophilic addition of in‐situ generated dithiocarbamates to allenoates in a rapid mild method using an eco‐friendly metal promoter. [ABSTRACT FROM AUTHOR]

Recently, inorganic anions and sulphonamides, two of the main classes of zinc-binding carbonic anhydrase inhibitors (CAIs), were investigated for inhibition of the α-class carbonic anhydrase (CA, EC 4.2.1.1) from Neisseria gonorrhoeae, NgCA. As an extension to our previous studies, we report that dithiocarbamates (DTCs) derived from primary or secondary amines constitute a class of efficient inhibitors of NgCA. KIs ranging between 83.7 and 827 nM were measured for a series of 31 DTCs that incorporated various aliphatic, aromatic, and heterocyclic scaffolds. A subset of DTCs were selected for antimicrobial testing against N. gonorrhoeae, and three molecules displayed minimum inhibitory concentration (MIC) values less than or equal to 8 µg/mL. As NgCA was recently validated as an antibacterial drug target, the DTCs may lead to development of novel antigonococcal agents. [ABSTRACT FROM AUTHOR]

Nowadays, cancer disease seems to be the second most common cause of death worldwide. Molecular hybridization is a drug design strategy that has provided promising results against multifactorial diseases, including cancer. In this work, two series of phthalazinone-dithiocarbamate hybrids were described, compounds 6–8, which display the dithiocarbamate scaffold at N2, and compounds 9, in which this moiety was placed at C4. The proposed compounds were successfully synthesized via the corresponding aminoalkyl phthalazinone derivatives and using a one-pot reaction with carbon disulfide, anhydrous H3PO4, and different benzyl or propargyl bromides. The antiproliferative effects of the titled compounds were explored against three human cancer cell lines (A2780, NCI-H460, and MCF-7). The preliminary results revealed significant differences in activity and selectivity depending on the dithiocarbamate moiety location. Thus, in general terms, compounds 6–8 displayed better activity against the A-2780 and MCF-7 cell lines, while most of the analogues of the 9 group were selective toward the NCI-H460 cell line. Compounds 6e, 8e, 6g, 9a–b, 9d, and 9g with IC50 values less than 10 µM were the most promising. The drug-likeness and toxicity properties of the novel phthalazinone-dithiocarbamate hybrids were predicted using Swiss-ADME and ProTox web servers, respectively. [ABSTRACT FROM AUTHOR]

Jie Guo,1,* Airen Xu,2,* Maojun Cheng,1 Yang Wan,1 Rikang Wang,1 Yuanying Fang,1 Yi Jin,1 Sai-Sai Xie,1 Jing Liu3 1National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Chinese Medicine, Nanchang, Jiangxi, People’s Republic of China; 2Clinical Pharmacology Research Center, The Second Hospital of Yinzhou, Ningbo, Zhejiang, People’s Republic of China; 3School of Pharmacy, Jiangxi University of Chinese Medicine, Nanchang, Jiangxi, People’s Republic of China*These authors contributed equally to this workCorrespondence: Sai-Sai Xie, National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Chinese Medicine, No. 56, Yangming Road, Donghu District, Nanchang City, Jiangxi Province, 330006, People’s Republic of China, Email xiesaisainanchang@hotmail.com Jing Liu, School of Pharmacy, Jiangxi University of Chinese Medicine, No. 56, Yangming Road, Donghu District, Nanchang City, Jiangxi Province, 330006, People’s Republic of China, Email liujing860828@163.comBackground: Alzheimer’s disease (AD) belongs to neurodegenerative disease, and the increasing number of AD patients has placed a heavy burden on society, which needs to be addressed urgently. ChEs/MAOs dual-target inhibitor has potential to treat AD according to reports.Purpose: To obtain effective multi-targeted agents for the treatment of AD, a novel series of hybrid compounds were designed and synthesized by fusing the pharmacophoric features of 3,4-dihydro-2 (1H)-quinolinone and dithiocarbamate.Methods: All compounds were evaluated for their inhibitory abilities of ChEs and MAOs. Then, further biological activities of the most promising candidate 3e were determined, including the ability to cross the blood-brain barrier (BBB), kinetics and molecular model analysis, cytotoxicity in vitro and acute toxicity studies in vivo.Results: Most compounds showed potent and clear inhibition to AChE and MAOs. Among them, compound 3e was considered to be the most effective and balanced inhibitor to both AChE and MAOs (IC50=0.28 μM to eeAChE; IC50=0.34 μM to hAChE; IC50=2.81 μM to hMAO-B; IC50=0.91 μM to hMAO-A). In addition, 3e showed mixed inhibition of hAChE and competitive inhibition of hMAO-B in the enzyme kinetic studies. Further studies indicated that 3e could penetrate the BBB and showed no toxicity on PC12 cells and HT-22 cells when the concentration of 3e was lower than 12.5 μM. More importantly, 3e lacked acute toxicity in mice even at high dose (2500 mg/kg, P.O.).Conclusion: This work indicated that compound 3e with a six-carbon atom linker and a piperidine moiety at terminal position was a promising candidate and was worthy of further study.Graphical Abstract: Keywords: Alzheimer’s disease, cholinesterase, monoamine oxidase, 3,4-dihydro-2(1H)-quinolinone, dithiocarbamate

Mild steel is a type of carbon steel with quite a low carbon content, or particularly known as plain-carbon steel. It is often used as a construction material because of its relatively low price. However, unlike stainless steel, it has low corrosion resistance, therefore some form of a protective film should be applied to prevent it from rusting in the corrosive environment. The inhibiting action of the synthesised dithiocarbamates (DTC), namely, Co(II) N-butylmethyldithiocarbamate, Co[BuMedtc]2 and Co(II) N-ethylbenzyldithiocarbamate, Co[EtBenzdtc]2 towards the corrosion behaviour of mild steel in acidic solution was studied. The proposed structures of complexes were characterised by using Fourier transform infrared (FTIR), ultraviolet-visible (UV-Vis), gravimetric analysis, molar conductivity, and melting point measurement. The analysis data deduced that the DTC ligands have successfully coordinated to Co(II) ion in a bidentate manner. The corrosion inhibition study showed that Co[BuMedtc]2 was a better corrosion inhibitor compared to Co[EtBenzdtc]2 because this is most likely due to the presence of a less bulky alkyl substituent (-CH3) in Cu[BuMedtc]2 and hence, showing great corrosion inhibition performance. Besides, the shorter the alkyl chain length in Cu[BuMedtc]2, the higher the solubility of the complex in the acid medium. The complexes showed better effectiveness in hydrochloric acid (HCl) rather than sulphuric acid (H2SO4) solution. The corrosion happened more actively in HCl than H2SO4 due to the chloride ions shown more destructive effect than sulfate ion on the carburised low carbon steel samples. In addition, when the concentration of inhibitor increases, the corrosion rate will be decreased.

[Display omitted] • Synthesis of 5-(hydoxymethyl)-1,3-thiazolidine-2-thiones is developed. • Fixation of carbon disulfide in N -alkyl(aryl) epoxy amines is carried out. • The reaction proceeds via intramolecular epoxide ring opening. • The products were obtained in good to high yields and excellent regioselectivity. An efficient method for the synthesis of 5-(hydoxymethyl)-1,3-thiazolidine-2-thiones is developed via the reaction of carbon disulfide with N -alkyl(aryl) epoxy amines. The reaction proceeds via intramolecular epoxide ring opening with in situ prepared dithiocarbamic acid. The products were obtained in good to high yields. [ABSTRACT FROM AUTHOR]

[Display omitted] • Two novel phthalazinone PARP-1 inhibitor (DLC-1 – 46) and dual PARP-1/HDAC-1 inhibitors (DLC-47 – 63) were designed and synthesized. • The synthesized compounds were tested in vitro for their PARP-1 and PARP/HDAC-1 activities. • Most compounds showed high inhibitory activity on PARP-1 enzyme, especially DLC-1 – 6 , which showed IC 50 value <0.2 nM, which was better than the positive drug Olaparib. • Several compounds exhibited potent dual-target inhibitory activity, with DLC-49 displaying IC 50 values of 0.53 nM and 17 nM for PARP-1 and HDAC-1, respectively. • DLC-50 demonstrated the most potent anti-proliferative activity, with IC 50 values for inhibiting the proliferation of MDA-MB-436, MDA-MB-231, and MCF-7 cells at 0.30, 2.70, and 2.41 μM. In recent years, poly(ADP-ribose)polymerase-1 (PARP-1) and histone deacetylase (HDAC) have emerged as significant targets in tumor therapy, garnering widespread attention. In this study, we designed and synthesized two novel phthalazinone PARP-1 inhibitors and dual PARP-1/HDAC-1 inhibitors, named DLC-1 – 46 containing dithiocarboxylate fragments and DLC-47 – 63 containing hydroxamic acid fragments, and evaluated their inhibitory activities on enzymes and cells. Among the PARP-1 inhibitors, most compounds exhibited high inhibitory activity against the PARP-1 enzyme, with DLC-1 – 6 being particularly notable, showing IC 50 values <0.2 nM. Notably, DLC-1 demonstrated significant anti-proliferative activity, with IC 50 values for inhibiting the proliferation of MDA-MB-436, MDA-MB-231, and MCF-7 cells reaching 0.08, 26.39, and 1.01 μM, respectively. Further investigation revealed that DLC-1 arrested MDA-MB-231 cells in the G1 phase and induced apoptosis in a dose-dependent manner. Among the designed dual PARP-1/HDAC-1 inhibitors, several compounds exhibited potent dual-target inhibitory activity, with DLC-49 displaying IC 50 values of 0.53 nM and 17 nM for PARP-1 and HDAC-1, respectively. DLC-50 demonstrated the most potent anti-proliferative activity, with IC 50 values for inhibiting the proliferation of MDA-MB-436, MDA-MB-231, and MCF-7 cells at 0.30, 2.70, and 2.41 μM, respectively. Cell cycle arrest and apoptosis assays indicated that DLC-50 arrested the cell cycle in the G2 phase and induced apoptosis in HCT-116 cells. Our findings present a novel avenue for further exploration of PARP-1 inhibitors and dual PARP-1/HDAC-1 inhibitors. [ABSTRACT FROM AUTHOR]

The hydrophobization mechanism of N -[(3-hydroxyamino)-propoxy]- N -octyl dithiocarbamate (OAHD) towards ilmenite. [Display omitted] • N -[(3-hydroxyamino)-propoxy]- N -octyl dithiocarbamate (OAHD) was pioneeringly introduced into the direct flotation of ilmenite as an efficient collector. • In situ AFM observed the self-assembled adsorption of OAHD on ilmenite surface. • OAHD's dithiocarbamate (−C(=S)-S−) and hydroxamate (–NH(C=O)O−) groups both chelated with the surface Fe(II) species on ilmenite. • The "h" configuration of OAHD adsorption model intensified the hydrophobicity of ilmenite, which strengthened its flotation recovery. • A green and efficient flotation process of ilmenite was realized. The pre-activation of lead nitrate has been extensively proved to be an effective technique in ilmenite flotation, and sodium oleate is the preferred collector. Realization the clean flotation of ilmenite is an important aspect to respond the green and low-carbon policy. In this work, a dithiocarbamate-hydroxamate collector OAHD was pioneeringly added into the direct flotation of ilmenite as an efficient collector. The micro-flotation performance found that OAHD realized an efficient flotation of ilmenite under low concentration of 1.0 × 10−5 mol/L under around pH 8.0, and the flotation recovery rate of ilmenite reached about 94.2%, which was about 35.8% higher than that of NaOL. The morphology of ilmenite observed by AFM probed the self-assemble adsorption behavior of OAHD on ilmenite surface. DFT (density functional theory) calculations suggested that both dithiocarbamate and hydroxamate groups are the chemical active centers and have strong electron acceptability of d-orbital electrons of Fe atoms at/on the interface of ilmenite. UV–Vis spectra demonstrated that dithiocarbamte and hydroxamate groups simultaneously has strong chemical reaction with Fe2+ ions. XPS analysis recommended that OAHD chemisorbed on ilmenite surface to produce the surface Fe(II)-OAHD complexes where the O,O-five membered ring of Fe(II)-hydroxamate compounds were formed. [ABSTRACT FROM AUTHOR]

[Display omitted] • New series of metallomacrocyclic complexes holding functionalized linkers. • Ability to act as single source precursors for the synthesis of MS nanoparticle. • HOMO-LUMO band gaps falls in the range of 1.19–1.33 eV for some of the complexes. • Potential molecular probes for optical detection of Pb(II), Cd(II) and Hg(II) ions. Two secondary diamines viz. N,N' -bis{3-(p -methoxybenzylamino)propyl}piperazine (H 2 L1) and N,N' -bis{3-(p-chlorobenzylamino)propyl}piperazine (H 2 L2) holding N,N' -bispropylpiperazine linkers have been prepared and subsequently used to derive a new series of N,N' -bis(3-dithiocarbamatopropyl) piperazine bridged metallomacrocyclic complexes [M(II) 2 - µ2 -bis-{(κ2S,S -S 2 CN(R)C 3 H 6) 2 piperazine}] wherein R = p -methoxybenzyl, M = Ni(II) 1, Cu(II) 2, Zn(II) 3; R = p -chlorobenzyl, M = Ni(II) 4, Cu(II) 5, Zn(II) 6. The formation and purity of all the metallomacrocyclic dithiocarbamate complexes were verified by microanalysis and standard methods such as HRMS, NMR, IR and UV–Visible absorption spectroscopy and corroborated by density functional theory calculations. The experimental (magnetic susceptibility and UV–Visible) and theoretical calculations suggest a square planar/distorted square planar environment around nickel(II)/copper(II) and tetrahedral/distorted tetrahedral environment around zinc(II) centres in 1–6. Thermogravimetric study was carried out on 1–6 to study their thermal stability and degradation behaviour. Notably, TG curves of compounds 2, 3 and 5 gave a stable residual mass corresponding to corresponding metal sulphides (MS). Notably, the calculated HOMO-LUMO gaps (1.19–1.33 eV) for Cu(II)-dithiocarbamate 2 and 5 indicates their semiconducting nature. The potentials of these metallomacrocycles as a molecular probe for optical sensing of environmentally hazardous heavy metal ions ca Pb(II), Cd(II) and Hg(II) were further examined by using UV–Visible and fluorescence spectroscopies. [ABSTRACT FROM AUTHOR]

Recently, inorganic anions and sulphonamides, two of the main classes of zinc-binding carbonic anhydrase inhibitors (CAIs), were investigated for inhibition of the α-class carbonic anhydrase (CA, EC 4.2.1.1) from Neisseria gonorrhoeae, NgCA. As an extension to our previous studies, we report that dithiocarbamates (DTCs) derived from primary or secondary amines constitute a class of efficient inhibitors of NgCA. KIs ranging between 83.7 and 827 nM were measured for a series of 31 DTCs that incorporated various aliphatic, aromatic, and heterocyclic scaffolds. A subset of DTCs were selected for antimicrobial testing against N. gonorrhoeae, and three molecules displayed minimum inhibitory concentration (MIC) values less than or equal to 8 µg/mL. As NgCA was recently validated as an antibacterial drug target, the DTCs may lead to development of novel antigonococcal agents.

The high theoretical ability of the tin sulfide (SnS) semiconductor makes it a potential material for solar cell applications. However, employing an environmentally friendly and cost-effective framework for the synthesis of SnS sustainable materials is essential. The attraction of the single-source precursor (SSP) route of preparing flexible nanostructured metal sulfide is due to its simplified procedures, high efficiency, fewer reagents and scale-up abilities. In this study, SSP route was used to prepare SnS nanoparticles with tunable sizes and better morphologies from three molecular precursors. XRD shows the structural characteristics of the three samples confirm the presence of orthorhombic phases for SnS1, SnS2 and SnS3. HRTEM images for SnS2 and SnS3 display irregular orthorhombic phases with an average size of 17.11 nm and 3.38–4.19 nm as compared to SnS1, which reveals a spherical structure and a grain size of 2.22–3.33 nm. There have been very few studies that have established nanorods SnS, but none from a single molecular precursor.

In industrial sectors, pickling and acid cleaning are mutual processes where acid solutions, such as hydrochloric acid (HCl) and sulfuric acid (H2SO4), are used to eliminate the corrosion products yielded on metal surfaces; thus, improving the performance of the machineries. However, the usage of the acid could lead to another metal deterioration. Dithiocarbamate inhibitor is defined as an organic compound that has good corrosion inhibition properties that can work as an inhibitor in an acid environment. Dithiocarbamate (DTC) assists by reducing acid reactiveness which prohibits metal dissolution in the acid. In this study, the Ni(II) N-butylmethyldithiocarbamate (Ni[BuMedtc]2) complex was synthesised by using an in-situ method and characterised by elemental analyser, attenuated total reflection Fourier transform infrared (ATR-FTIR), ultraviolet-visible (UV-Vis) spectroscopy and X-ray crystallographic study, and the chemical properties of the Ni[BuMedtc]2 complex was successfully calculated by the Discrete Fourier Transform (DFT) approach. The experimental results which were obtained through the weight-loss analysis method in two different acids – 1 M HCl and 1 M H2SO4 – indicated that the inhibition efficiency increased as the inhibitor concentration increased. The outcome showed that the Ni[BuMedtc]2 performed better as an inhibitor in 1 M HCl as compared to in1 M H2SO4 to protect the metal exterior because H2SO4 is more corrosive due to the excessive presence of H+.

To develop novel radiolabeled amino acid tumor imaging agents, 4-methoxy-L-phenylalanine dithiocarbamate (MOPADTC) was synthesized successfully, and two kinds of 99mTc-labeled complexes ([99mTc]TcN-MOPADTC and [99mTc]TcO-MOPADTC) with high radiochemical purities (RCP > 95%) were obtained. The in vitro stability and partition coefficient were determined, and the results show that both of these complexes have good in vitro stability; [99mTc]TcO-MOPADTC is hydrophilic, while [99mTc]TcN-MOPADTC is slightly lipophilic. The biodistribution of [99mTc]TcN-MOPADTC and [99mTc]TcO-MOPADTC in mice bearing S180 tumors shows that the tumor uptake and tumor/muscle ratio of [99mTc]TcO-MOPADTC were higher than the tumor uptake and tumor/muscle ratio of [99mTc]TcN-MOPADTC. In addition, the tumor retention of [99mTc]TcO-MOPADTC is better than the tumor retention of [99mTc]TcN-MOPADTC. A competitive inhibition assay was performed, and the results indicate that [99mTc]TcO-MOPADTC may enter cells primarily via the L-alanine/L-serine/L-cysteine (ASC) system. Single-photon emission computed tomography (SPECT) imaging of [99mTc]TcO-MOPADTC shows obvious accumulation in tumor sites, suggesting that [99mTc]TcO-MOPADTC is a novel potential tumor-imaging agent. [ABSTRACT FROM AUTHOR]

Dithiocarbamates constitute an important class of broad-spectrum antifungal compounds used extensively in agriculture, including in the cultivation of spices. Maximum residue limits for these compounds have been enforced by several importing countries in international food trade. Validation of analytical methods for dithiocarbamates in spices have not been reported previously. A quick and sensitive method for estimation of total dithiocarbamates as carbon disulphide (CS2) using GC-MS in two major spices, viz. small cardamom (Elettaria cardamomom) and black pepper (Piper nigrum) was optimized and validated. Dithiocarbamate residues in these spice matrices were extracted and subjected to acid hydrolysis followed by reduction to CS2, which was then quantitatively absorbed into isooctane and analysed using GC-MS, employing selected ion monitoring and post-run mid-column backflush technique. For fortification levels from 0.1 to 1.0 mg kg− 1, recoveries obtained ranged from 75 to 98% in cardamom and 76–98% in black pepper, with intra-day precision (RSDr) < 12% and inter-day precision (RSDR) < 15% in all cases. Limit of Quantification of 0.05 mg kg− 1 was achieved in both spices. It was found that there was negligible interference in quantitative accuracy due to essential oils present in the two spices studied. Matrix effect was seen to be suppressive in the two spices studied, and sufficiently low to exclude the use of matrix-matched calibration in routine quantitative analysis. The optimized analytical method was found to be suitable for evaluation of compliance of real samples against the Codex maximum residue limits for cardamom and black pepper. Safety evaluation for human consumption, based on the incidence of Dithiocarbamate residues, was performed in real samples of cardamom and black pepper. This method offers the possibility of extending applicability to other spices also. [ABSTRACT FROM AUTHOR]

In this work, a new strategy by in situ combining slag-based geopolymer microsphere (SGS) with dithiocarbamate (DTC) was employed to synthesize in situ the composite adsorbent of the SGS and DTC (SGS-DTC). The differences of material properties, performance, and mechanisms in adsorption and immobilization of toxic Cd(II) in water between the SGS and SGS-DTC were investigated. For the static adsorption, the adsorption rate of SGS-DTC(1.5h) was faster than that of SGS(6h); the Cd(II) adsorption capacity of the SGS-DTC (211.2 mg/g) was almost twice that of the SGS (116.7 mg/g), corresponding to the removal rate of the SGS-DTC (99.75%) was nearly twice that of the SGS (53.2%). For the dynamic adsorption, the adsorption capacity of the SGS-DTC is higher than that of the SGS in the Cd(II) solution prepared by the deionized water or the river water from Yongjiang, Nanning, Guangxi, China. The mechanism of the difference of the Cd(II) adsorption between SGS and SGS-DTC was analyzed in dept. [Display omitted] In this study, slag-based geopolymer microspheres (SGS) were combined with dithiocarbamate (DTC) to synthesize the composite adsorbent of SGS and DTC in situ (SGS-DTC). Synthesis was carried out with optimal dosages of 10 mL of EDA, 1.0 g of SGS, and 20 mL of CS 2. The differences in material properties, performance, and mechanisms in the adsorption and immobilization of toxic Cd(II) in water between SGS and SGS-DTC were investigated. SGS-DTC showed better adsorption performance than SGS, irrespective of adsorbent dosage, pH, original content, and contact duration. Although after the Cd(II) adsorption, the immobilization performance at a different pH was better in the SGS-DTC than in the SGS, the immobilization performance was unaffected by changes in the other factors. For static adsorption, the adsorption rate of SGS-DTC (1.5 h) was faster than that of SGS (6 h); the Cd(II) adsorption capacity of SGS-DTC (211.2 mg/g) was almost twice that of SGS (116.7 mg/g), and correspondingly, the removal rate of SGS-DTC (99.75%) was nearly twice that of SGS (53.2%). For dynamic adsorption, the adsorption capacity of SGS-DTC was 389.78 mg/g, which is considerably higher than that of SGS (293.38 mg/g) in the Cd(II) solution prepared with deionized water. Furthermore, the adsorption capacity of the SGS-DTC was 299.26 mg/g, which is significantly higher than that of SGS (150.03 mg/g) in the Cd(II) solution prepared by the river water from Yongjiang, Nanning, Guangxi, China. One reason is that DTC was able to activate Si-O-Si without adsorption performance within SGS, thereby improving its adsorption and purification properties significantly. The other reason is that, after anchoring DTC on SGS, the specific surface area varied from 34.05–146.47 m2/g, the morphology was smooth-leaf-like, the pore volume was 0.13–0.20 cm3/g, and the pore size in SGS, was 14.75–5.60 nm. The high potential of SGS-DTC in removing and immobilizing heavy metal materials in wastewater is demonstrated in the results. [ABSTRACT FROM AUTHOR]

In continuation of our interest in identifying new α-glucosidase inhibitors with potential to become antidiabetic drugs, this work focuses on the study of 4-(dimethylaminoalkyl)piperazine-1-carbodithioate derivatives as α-glucosidase inhibitors. The eight heterocyclic piperazine-dithiocarbamate complexes studied in this work contain a variety of substitutions on their benzene ring exhibiting potent, noncompetitive inhibition of α-glucosidase. Dithiocarbamate and piperazine moieties are important pharmacophores with promising therapeutic prospects featuring facilitated drug delivery due to their lipophilic nature in addition to their α-glucosidase inhibitory activity. Enzyme kinetics, molecular dynamics simulations, and docking studies revealed that the target compounds bind to a new allosteric site that is located near the active site of α-glucosidase. Majority of molecular interactions of the compounds with the enzyme are mediated by hydrophobic contacts in addition to a number of important polar interactions. The current work identifies a number of chemical groups in the compounds that are responsible for potent inhibition of α-glucosidase. Moreover, it also provides new insights into understanding α-glucosidase inhibition by dithiocarbamate and piperazine-containing compounds that can be promising for development of new antidiabetic drugs. [ABSTRACT FROM AUTHOR]

Vine leaves, which are produced fresh, brined or fermented from the leaves of Vitis Vinifera in Türkiye are an important food. Sulfur is used as a pesticide and sulfur compounds can be used as additives during the growing and processing of the vine leaves. These sulfur sources cause positive results on carbon disulfide (CS2) measurements by GC-MS. Therefore, the main objective of the present study was to investigate the effects of residues of sulfur or sulfur compounds on dithiocarbamate analysis methods based on CS2 measurement. For this, vine leaves were produced by controlled agricultural production and processed as brine under controlled conditions. The sulfur dioxide (SO2) and dithiocarbamate analysis were carried out on the vine leave obtained by applying sulfur spraying in agricultural treatments and brined vine leaves produced by adding sodium metabisulfite (SM), and control samples of each stage. SO2 was not detected in any of the samples in this study. SO2 residues did not occur in the vine leaves as a result of the sulfur spraying application and therefore did not have a false positive effect on dithiocarbamate analysis. However, approximately 0.15 mg kg−1 false positive dithiocarbamate was detected, which is thought to originate from natural sulfur in the vine leaves. The effect of SM, which was used in low concentration in the production of brined vine leaves, on dithiocarbamate results was limited. Even if SM was not used, the total false positive dithiocarbamate result in the brined vine leaves production process was approximately determined as 0.20 mg kg−1. This study showed that the dithiocarbamates analysis method based on CS2 measurement may lead to false positive results in brined vine leaves since sulfur compounds are found naturally in vine leaves. [ABSTRACT FROM AUTHOR]

Glycyrrhetinic acid (GA) is a naturally occurring triterpene compound. The aim of this study was to employ the pharmacophore hybrid strategy to merge GA with various dithiocarbamates and obtain novel compounds with better antitumor activities. We present a two-step synthetic protocol wherein the GA derivative underwent reaction with carbon disulfide and various secondary amines in a one-pot manner under mild conditions, facilitating the preparation of a series of structurally novel GA-dithiocarbamate derivatives. Bioassay screening revealed that the representative compound 3c demonstrated the capacity to reduce the mitochondrial membrane potential in Hep3B and Huh-7 cells, induce nuclear apoptosis, inhibit invasion and migration, and prompt both early and late apoptosis. Furthermore, our research findings indicated that this apoptotic phenomenon may be associated with the expression of Bcl-2, Bax, Bak, PARP, and cleaved-PARP proteins. Utilizing network pharmacology for predicting core targets and signaling pathways of compound 3c for hepatocellular carcinoma (HCC) treatment involved employing molecular docking models to demonstrate high affinity between compound and target protein. In conjunction with Western blot analysis, compound 3c may impact HCC through the PI3K-AKT-mTOR pathway., (© 2024 Deutsche Pharmazeutische Gesellschaft.)

A series of (C^S)-cyclometallated Au(III) cationic complexes of general formula [Au(dppta)(dtc)] + , [Au(dppta)(azmtd)] + and [Au(dppta)(azc)Cl] + (dppta = N,N-diisopropyl-P,P-diphenylphosphinothioic amide-κ 2 C,S; dtc = dithiocarbamate-κ 2 S,S'; azc = azolium-2-dithiocarboxylate-κ 1 S; azmdt = azol(in)ium-2-(methoxy)methanedithiol-κ 2 S,S') were synthetized and tested against a panel of bacterial strains belonging to different Gram-positive and Gram-negative species of the ESKAPE group of pathogens. Among the tested compounds, complex 4c had the higher Therapeutic Index (TI) against multidrug resistant strains of S. aureus, S. epidermidis and A. baumannii, showing a more favourable cytotoxicity profile than the reference gold metalloantibiotic Auranofin. © 2024 xxxxxxxx. Hosting by Elsevier B.V. All rights reserved., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Sara M. Soto has patent A gold(III) complex, a conjugate of the gold(III) complex, a pharmaceutical composition comprising the gold(III) complex and uses and a process for preparing the gold(III) complex issued to Institute of Global Health of Barcelona. If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 The Authors. Published by Elsevier Inc. All rights reserved.)

Most industries used acids during the cleaning process where they may cause a severe corrosion attack to the metal surface. Corrosion inhibitor was utilized to reduce the corrosion rate. Cobalt(II) N-methylcyclohexylamine dithiocarbamate, Co[MeCycHexdtc]2 and Cobalt(II) N-ethylcyclohexylamine dithiocarbamate, Co[EtCycHexdtc]2 were synthesized by using the in-situ method with a molar ratio of 2:2:1 (carbon disulphide:amine:metal salt) in cold ethanolic solution and characterized by using the Fourier Transform Infrared-Attenuated Total Reflectance (FTIR-ATR) and Ultraviolet-Visible (UV-Vis) spectroscopies. In the FTIR-ATR analysis, the presence of dithiocarbamate moiety was proven by the data shown with the presence of a new specific stretching bands, thioureide band, υ(C N) which is found in the range of 1478–1481 cm-1 and υ(C S) in 1010-1012 cm-1 of the spectra in both complexes. For UV-Vis analysis, the Co(II) dithiocarbamate complexes showed two transitions, πàπ* and nàπ* transitions, which indicated that the coordination between metal ions and dithiocarbamates ligands has successfully formed. The presence of peaks above 400 nm confirmed the d-d transition of Co(II) dithiocarbamate complexes. Furthermore, the corrosion inhibition screening of mild steel was studied for different corrosive media (1 M HCl and 1 M H2SO4) with and without different concentrations of the inhibitor. As the inhibitor concentration increased, the efficiency of the corrosion inhibitor also increased at a constant temperature.

In the present study, novel representatives of the important group of biologically-active, dehydroabietic acid-bearing dithiocarbamate moiety, were synthesized and characterized by 1H NMR, 13C NMR, HR-MS. The in vitro antiproliferative activity evaluation (MTT) indicated that these compounds exhibited potent inhibitory activities in various cancer cell lines (HepG-2, MCF-7, HeLa, T-24, MGC-803). Particularly, compound III-b possessed extraordinary cytotoxicity with low micromolar IC50 values ranging from 4.07 to 38.84 µM against tested cancer cell lines, while displayed weak cytotoxicity on two normal cell lines (LO-2 and HEK 293 T). Subsequently, the potential mechanisms of representative compound III-b were elementarily investigated by Transwell experiment, which showed III-b can inhibit cancer cells migration. Annexin-V/PI dual staining showed that the compound can induce HepG-2 cells apoptosis in a dose-dependent manner. Meanwhile this apoptosis may be related to the upregulated protein expression of cleaved-caspase 3, cleaved-caspase 9, Bax and downregulated of Bcl-2 indicated by Western Blot. Later study further confirmed that ROS levels in HepG-2 cells increased significantly with the rise of concentrations. In addition, through the network pharmacology data analyzing, the core targets and signaling pathways of compound III-b for treatment of liver neoplasms were forecasted. Molecular docking model showed that compound III-b had high affinity with hub targets (CASP3, EGFR, HSP90AA1, MAPK1, ERBB2, MDM2), suggesting that compound III-b might target the hub protein to modulate signaling activity. Taken together, these data indicated that dehydroabietic acid structural modification following the “Molecular hybridization” principle is a feasible way to discover the potential multi-targeted antitumor compounds.

An efficient and facile one-pot, five-component reaction for the synthesis of 2,6-diamino-1-alkyl-2-oxospiro[indoline-3,4′-thiopyran]-3,5-dicarbonitrile derivatives has been reported by a reaction between primary amines, carbon disulfide, malononitrile, and isatin derivatives. The major advantages of this procedure are high yields of products in relatively short reaction time, scalability, mild conditions, multi-component synthetic procedure, low catalyst loading, no column separation and simple reaction work-up. As a consequence, this synthetic procedure provided an efficient access to spirooxindole-annulated thiopyran derivatives.

Organotin (IV) dithiocarbamate has recently received attention as a therapeutic agent among organotin (IV) compounds. The individual properties of the organotin (IV) and dithiocarbamate moieties in the hybrid complex form a synergy of action that stimulates increased biological activity. Organotin (IV) components have been shown to play a crucial role in cytotoxicity. The biological effects of organotin compounds are believed to be influenced by the number of Sn-C bonds and the number and nature of alkyl or aryl substituents within the organotin structure. Ligands target and react with molecules while preventing unwanted changes in the biomolecules. Organotin (IV) dithiocarbamate compounds have also been shown to have a broad range of cellular, biochemical, and molecular effects, with their toxicity largely determined by their structure. Continuing the investigation of the cytotoxicity of organotin (IV) dithiocarbamates, this mini-review delves into the appropriate method for synthesis and discusses the elemental and spectroscopic analyses and potential cytotoxic effects of these compounds from articles published since 2010.

Chemiresistive composites of gold (Au) nanoparticles interlinked with different types of organic molecules were prepared automatically by layer-by-layer self-assembly using a microfluidic cell. For the assembly process, dodecylamine-stabilized Au nanoparticles with an average size of 3.7 nm as well as alkyl dithiols, alkyl diamines, and alkyl bisdithiocarbamates with different alkyl chain length (C6 and C8) were used. X-ray photoelectron spectroscopy was applied on prepared nanoparticle composites to study the film composition and the degree of interlinkage. For the measurement of electrical and vapor-sensing properties, silicon dies equipped with gold interdigitated electrodes were used. All films show linear current-voltage characteristics and conductivities in the range of 10-2 and 10-4 Ω-1 cm-1 at room temperature. The sensitivity of the film is investigated by dosing them with vapors of toluene, 1-propanol, 4-methyl-2-pentanone, and water in the concentration range from 100 to 5,000 ppm at 0% relative humidity. All composite films respond with an increase in their electrical resistance to the analytes. The sensors show a high signal-to-noise ratio which indicates a detection limit below 100 ppm for all test vapors. The response dynamics demonstrate a high reversibility and a fast sensing mechanism especially for dithiols and diamines with response and recovery times from 2 to 10 s. The dithiol sensors exhibit a high selectivity to toluene and 4-methyl-2-pentanone whereas the bisdithiocarbamate composites are suitable for the detection of water and 1-propanol. All materials are stable for (at least) several months. [ABSTRACT FROM AUTHOR]

Copper-catalyzed direct C(sp2)–H sulfuration of aryl alkenes by using tetraalkylthiuram disulfides as sulfuration reagents has been developed. The reaction provides an efficient method for the synthesis of a variety of alkenyl dithiocarbamates, which are important structure motifs widely applied in materials, pharmaceuticals, and agrochemicals. [ABSTRACT FROM AUTHOR]

The pressure‐induced transformation of plane‐square complex nickel(II) bis(N,N‐diethyldithiocarbamate) between its soft dithiocarbamate (form I) and thioureide (form II) mesomeres is coupled to the interchange of anagostic Ni⋅⋅⋅H−C interactions from methylene to the methyl group, respectively. At 1.23 GPa, the clearly visible giant anomalous compressibility of the crystal reveals a potential‐energy difference of 5.4 kJ mol−1 between the two complex forms. The structural and spectroscopic results, which are supported by quantum‐mechanical calculations, connect this solid‐state phase transition with the mesomeric transition, and this is accompanied by the conformational transformation of anagostic Ni⋅⋅⋅H−C rearrangement and formation of the charge‐assisted S−⋅⋅⋅H−C bond under pressure. [ABSTRACT FROM AUTHOR]

Triphenylarsenic(V) mixed ligand derivatives; [(R1)(R2)C=NO]2[Ph]3As[S2CN(CH2CH2)2O] (1 A‐1F) were synthesized [Where R1=−C6H5, R2=−CH3(1 A); R1=−C6H4CH3, R2=−CH3(1 B); R1=−C6H4Cl, R2=−CH3(1 C); R1=−C6H4Br, R2=−CH3(1 D); R1=−C6H4OH, R2=−H(1 E); R1(R2)C=C−CH2−(CH2)3−CH2 (1 F)] by consecutive substitution of Ph3AsBr2 with sodium salt of substituted oximes and morpholinedithiocarbamate in equimolar proportion. Distorted octahedral geometry was proposed around the arsenic atom, for these derivatives. Nano ranged particle size ∼35 nm with crystalline nature was obtained by powder XRD study for these derivatives. The derivatives were examined for bacteria and fungi which exhibited higher antifungal capability than antibacterial. Cytotoxic and antioxidant activities were performed through MTT test in 3T3 fibroblast cell lines and by FRAP assay, respectively for these derivatives. Amongst six triphenylarsenic(V) mixed ligand derivatives, 1 A, 1 B and 1 C were observed non‐noxious (cell viability >50 % even at 500 μg/mL) in nature and 1 D, 1 E and 1 F were poisonous to 3T3 fibroblast cell lines. Structural‐Activity relationship for antimicrobial and antioxidant activity amongst six derivatives 1 A–1 F was explored. [ABSTRACT FROM AUTHOR]

Homoleptic pyridyl-3(N) functionalized dithiocarbamate complexes namely, [Zn(L1)2]21 (L1 = (C5H4NCH2)2NCS2) and [Cd(L2)2] ∞2 (L2 = CH3C6H4CH2NCS2CH2C4H3O) have been synthesized and characterized by elemental analysis and different spectroscopic techniques. Single crystal structural studies reveal that compound 1 is binuclear while, 2 is polymeric structure. The presence of weak interactions between complexes and solvent molecules in the lattice results in one-dimensional and three-dimensional supramolecular structures of 1 and 2 respectively. In the case of complex 2, a rare and significant S···Cl chalcogen bonding interaction was found, which involve the solvent molecule in chain motifs. Complex 2 is a unique example of homoleptic metal dithiocarbamate complexes exhibiting such types of interactions. Complexes showed emission in the solid state. The TGA studies of complexes revealed that complex 1 would be a good precursor for the preparation of ZnS thin film via metal organic chemical vapor deposition (MOCVD). [ABSTRACT FROM AUTHOR]

Two new families of dithiocarbamate gold(I) complexes derived from benzenesulfonamide with phosphine or carbene as ancillary ligands have been synthesized and characterized. In the screening of their in vitro activity on human colon carcinoma cells (Caco-2), we found that the more lipophilic complexes—those with the phosphine PPh3—exhibited the highest anticancer activity whilst also displaying significant cancer cell selectivity. [Au(S2CNHSO2C6H5)(PPh3)] (1) and [Au(S2CNHSO2-p-Me-C6H4)(IMePropargyl)] (8) produce cell death, probably by intrinsic apoptosis (mitochondrial membrane potential modification) and caspase 3 activation, causing cell cycle arrest in the G1 phase with p53 activation. Besides this, both complexes might act as multi-target anticancer drugs, as they inhibit the activity of the enzymes thioredoxin reductase (TrxR) and carbonic anhydrase (CA IX) with the alteration of the redox balance, and show a pro-oxidant effect. [ABSTRACT FROM AUTHOR]

• Palladium(II) (1,2) and platinum(II) (3,4) long chain dithiocarbamate complexes were prepared. • X-ray analysis of 1 and 4 revealed the square planar coordination geometry around the metal centre. • Complex 4 revealed intermolecular anagostic C-H∙∙∙Pt interactions. • C-H∙∙∙Pt interactions were characterized using DFT, Hirshfeld surface analysis and AIM analysis. • Platinum complexes (3,4) show better anticancer activity than those of palladium complexes (1,2). Four new homoleptic complexes bis(N-dodecyl-N-benzyl)dithiocarbamato-S,S')M(II) (where M=palladium (1), platinum (3)) and bis(N-dodecyl-N-(2-hydroxybenzyl)dithiocarbamato-S,S')M(II) (where M=palladium (2), platinum (4)) were synthesized and characterized using elemental analysis, FTIR and NMR spectra. The crystal structures of 1 and 4 were solved by single crystal X-ray diffraction technique. Single crystal X-ray analysis of the two of the complexes (1 and 4) revealed the presence of a distorted square planar coordination geometry (S 4) about the metal centre. Complex 4 revealed two intermolecular anagostic C-H∙∙∙Pt interactions which were characterized through a comprehensive set analysis using single crystal X-ray diffraction (experimental) and DFT, Hirshfeld surface analysis and AIM (theoretical) analysis. The electronic behavior, MEP surfaces, FMO and DOS studies of the complexes 1 and 4 were investigated employing DFT. A strong correlation has been found between both experimental and theoretical bond parameters. MTT assay was used to study the antitumor activities of 1 – 4 against MCF7 cancer cells. The results reveal that all complexes have fine anticancer activities. [Display omitted] [ABSTRACT FROM AUTHOR]

A series of (C^S)-cyclometallated Au(III) cationic complexes of general formula [Au(dppta)(dtc)]+, [Au(dppta)(azmtd)]+ and [Au(dppta)(azc)Cl]+ (dppta = N,N-diisopropyl- P , P -diphenylphosphinothioic amide-κ2C,S; dtc = dithiocarbamate-κ2S,S′; azc = azolium-2-dithiocarboxylate-κ1S; azmdt = azol(in)ium-2-(methoxy)methanedithiol-κ2S,S′) were synthetized and tested against a panel of bacterial strains belonging to different Gram-positive and Gram-negative species of the ESKAPE group of pathogens. Among the tested compounds, complex 4c had the higher Therapeutic Index (TI) against multidrug resistant strains of S. aureus , S. epidermidis and A. baumannii , showing a more favourable cytotoxicity profile than the reference gold metalloantibiotic Auranofin. © 2024 xxxxxxxx. Hosting by Elsevier B.V. All rights reserved. In this work, we report a series of (C^S)-cyclometallated gold(III) cationic complexes with potent antibacterial activity against different species of clinically relevant Gram-positive and Gram-negative pathogenic bacteria. Importantly, a complex exhibiting low cytotoxicity towards mammalian cells was found, indicating high selectivity. [Display omitted] • Cyclometallated gold(III) cationic complexes display potent antibacterial activity. • Gold(III) cationic complexes show selectivity for Gram-positive strains. • However, they also display remarkable activity against Gram-negative A. baumannii. • The ligands are suitable to stabilize gold(III) under physiological conditions. • A complex exhibiting low cytotoxicity towards mammalian cells was found. [ABSTRACT FROM AUTHOR]

Novel phenothiazine-dithiocarbamate analogues were designed by molecular hybridization strategy and synthesized and evaluated for their anticancer activity in vitro against three selected cancer cell lines (EC-109, MGC-803, and PC-3). The preliminary structure-activity relationship (SAR) for this phenothiazine-dithiocarbamate hybrids is explored. Among all analogues, 2-oxo-2-(10H-phenothiazin-10-yl)ethyl 4-ethylpiperazine-1-carbodithioate (8a) showed the most potent inhibitory activity with an [Formula: see text] value of [Formula: see text] against PC-3 cells. In addition, compound 8a could arrest the cell cycle at the G1 phase and regulate the expression of G1 checkpoint-related proteins, suggesting that phenothiazine-dithiocarbamate hybrids might be useful as cell cycle blockers.

Chemiresistive composites of gold (Au) nanoparticles interlinked with different types of organic molecules were prepared automatically by layer-by-layer self-assembly using a microfluidic cell. For the assembly process, dodecylamine-stabilized Au nanoparticles with an average size of 3.7 nm as well as alkyl dithiols, alkyl diamines, and alkyl bisdithiocarbamates with different alkyl chain length (C6 and C8) were used. X-ray photoelectron spectroscopy was applied on prepared nanoparticle composites to study the film composition and the degree of interlinkage. For the measurement of electrical and vapor-sensing properties, silicon dies equipped with gold interdigitated electrodes were used. All films show linear current-voltage characteristics and conductivities in the range of 10–2 and 10–4 Ω−1 cm−1 at room temperature. The sensitivity of the film is investigated by dosing them with vapors of toluene, 1-propanol, 4-methyl-2-pentanone, and water in the concentration range from 100 to 5,000 ppm at 0% relative humidity. All composite films respond with an increase in their electrical resistance to the analytes. The sensors show a high signal-to-noise ratio which indicates a detection limit below 100 ppm for all test vapors. The response dynamics demonstrate a high reversibility and a fast sensing mechanism especially for dithiols and diamines with response and recovery times from 2 to 10 s. The dithiol sensors exhibit a high selectivity to toluene and 4-methyl-2-pentanone whereas the bisdithiocarbamate composites are suitable for the detection of water and 1-propanol. All materials are stable for (at least) several months.

A metal-free multicomponent synthetic route for the diverse preparation of dithiocarbamate-containing piperazine derivatives was developed through the C–N bond cleavage of DABCO ring. This multicomponent re-engineering approach proceeds via the reaction of amines, CS2 and DABCO salts in one pot. Various DABCO salts and secondary amines are tolerated well in this protocol to afford a broad spectrum of dithiocarbamate-containing piperazines in good to high yields. Then, the selected compounds have been deployed against some critical types of bacteria and fungi. A certain number of synthesized compounds revealed not only appropriate antibacterial activity as investigated by disc fusion and minimum inhibitory concentration methods against bacteria (Gram-positive and Gram-negative), but also depicted good to excellent antifungal activity.

An efficient method for the synthesis of highly substituted bicyclic pyridone derivatives containing the dithiocarbamate group is reported via a one-pot three-component reaction of 2-(alkylthio)thio­azlactones, diamines, and nitroketene dithioacetal in EtOH under catalyst-free conditions. The reaction proceeds via a domino amidation–­intramolecular 1,4-addition-type Friedel–Crafts alkylation reaction to afford the corresponding fused bicyclic pyridones with high yields and diastereoselectivity.

Mild steel plays an essential part in many construction industries due to its low cost and excellent mechanical properties. However, the use of strong acid in pickling, construction, and oil refining processes adds to a serious corrosion problem for mild steel. Two Cu(II) dithiocarbamate complexes were successfully synthesized, namely Cu[EtBenzdtc]2 and Cu[BuMedtc]2 by condensation to scrutinize the corrosion resistance activity toward mild steel in acidic media. The proposed structures of complexes were characterized using Fourier transform infrared (FTIR) and ultraviolet-visible (UV-Vis) spectroscopies. The melting point for Cu[EtBenzdtc]2 was found around 362–375 °C and 389–392 °C for Cu[BuMedtc]2. The percentages of Cu (II) found in Cu[EtBenzdtc]2 and Cu[BuMedtc]2 are 7.6% and 7.5%, respectively. Both complexes were non-electrolyte based on the molar conductivity analysis. Their corrosion inhibition performances were tested by a weight loss measurement. Cu[BuMedtc]2 showed a good result as a corrosion inhibitor compared to Cu[EtBenzdtc]2. The complexes showed good effectiveness in sulfuric acid (H2SO4) compared to hydrochloric acid (HCl) solution.

• Synthesis of sulfonated piperazine derivatives containing dithiocarbamate group is developed. • The reaction proceeds via DABCO C N bond cleavage. • Quaternized DABCO salts were synthesized using sultones. • The products revealed acceptable antibacterial activity. • Some of the ensured products simultaneously demonstrated anti -glioma effects. A catalyst-free synthetic route for the diversity-oriented synthesis of sulfonated piperazine derivatives containing dithiocarbamates, thiol and azide functional groups was developed via DABCO C N bond cleavage. In this synthetic strategy, quaternized DABCO salts were synthesized using sultones and reacted with various nucleophiles namely dithiocarbamates, thiols and sodium azide to afford the target functionalized sulfonated piperazines derivatives in moderate to excellent yields. It is the first report on using sultones as activating agents for DABCO bond cleavage. Finally, the ensued products revealed acceptable antibacterial activity as examined by disk fusion and microdilution methods against both Gram-positive and Gram-negative bacteria like S. aureus and E. coli. More importantly, some of the ensured products simultaneously demonstrated anti -glioma effects with a negligible killing effect on mammalian cells. [Display omitted] [ABSTRACT FROM AUTHOR]

• Two rare examples of dithiocarbamates derivative complexes of Os, i.e. a trithiocarbamate-dithiocarbamate complex cis -[Os(CO) 2 (S 2 CNMe 2)(S 3 CNMe 2)] (2) and a binuclear [Os 2 (CO) 3 (S 2 CNMe 2) 2 (µ-CNMe 2)(µ-SCNMe 2)] (3) that contains dithiocarbamate, thiocarboxamide and amino-carbyne ligands. • Examples of sulfur insertion into an Os-S bond of cis -[Os(CO) 2 (S 2 CNMe 2) 2 ] (1) and the oxidative addition of a C-S bond in Me 4 TMS. • Crystal structures for all new osmium complexes Thermolytic reactions of [Os 3 (CO) 12 ] with tetramethylthiuram disulfide (Me 4 TDS) and tetramethylthiuram monosulfide (Me 4 TMS) are described. While both afford the anticipated bis(dithiocarbamate) complex cis -[Os(CO) 2 (S 2 CNMe 2) 2 ] (1) as the major product, unexpected secondary products result in both cases. With Me 4 TDS this is the trithiocarbamate-dithiocarbamate complex cis -[Os(CO) 2 (S 2 CNMe 2)(S 3 CNMe 2)] (2) resulting (formally) from sulfur insertion into an Os-S bond. Heating 1 with further Me 4 TDS did afford 2 , albeit in small amounts and on a timeframe incompatible with its formation under the initial reaction conditions. From the Me 4 TMS reaction, binuclear [Os 2 (CO) 3 (S 2 CNMe 2) 2 (µ-CNMe 2)(µ-SCNMe 2)] (3) is a secondary product. It contains dithiocarbamate, thiocarboxamide and amino-carbyne ligands, the last two resulting (formally) from the oxidative addition of a C-S bond in Me 4 TMS. Both new complexes have been characterised by X-ray crystallography. [Display omitted] [ABSTRACT FROM AUTHOR]

In this paper, novel gold(I) N -heterocyclic carbene with DTC and alkynyl complexes were synthesized. The gold(I) NHC with DTC complexes showed good to excellent antiproliferative activity and were powerful inhibitors of TrxR. [Display omitted] • New gold(I) N -heterocyclic carbene with DTC and alkynyl complexes were synthesized. • The gold(I) NHC with DTC complexes showed good to excellent antiproliferative activity. • The gold(I) NHC with DTC complexes strongly inhibited TrxR. A series of new type gold(I) N -heterocyclic carbene (NHC) complexes bearing a paeonol ligand in the side chain of NHC and bearing dithiocarbamate or alkynyl groups as a second ligand have been synthesized and structurally characterized by spectroscopic methods. The structure of Pa-NHC-Au-Cl has been established by X-ray crystallography. Their antitumor activities in vitro were investigated by CCK8 assay against two tumor cell lines (A549 and Hela). The gold(I) NHC with dithiocarbamate (DTC) complexes showed good to excellent antiproliferative activity and strongly inhibited the selenoenzyme thioredoxin reductase (TrxR). [ABSTRACT FROM AUTHOR]

The discovery of cisplatin has influenced scientists to study the anticancer properties of other metal complexes. Organotin(IV) dithiocarbamate compounds are gaining attention as anticancer agents due to their potent cytotoxic properties on cancer cells. In this study, a series of organotin compounds were assessed for their toxic effects on the Jurkat E6.1 cell line. WST-1 assay was used to determine the cytotoxic effect of the compounds and showed that six out of seven organotin(IV) dithiocarbamate compounds exhibited potent cytotoxic effects toward T-lymphoblastic leukemia cells, Jurkat E6.1 with the concentration of IC50 ranging from 0.67–0.94 µM. The apoptosis assay by Annexin V-FITC/PI staining showed that all tested compounds induced cell death mainly via apoptosis. Cell cycle analysis assessed using RNase/PI staining showed that organotin(IV) dithiocarbamate compounds induced cell cycle arrest at different phases. In conclusion, the tested organotin(IV) dithiocarbamate compounds demonstrated potent cytotoxicity against Jurkat E6.1 cells via apoptosis and cell cycle arrest at low IC50 value. However, further studies on the mechanisms of action are required to probe the possible potential of these compounds on leukemia cells before they can be developed into anti-leukemic agents.

Mixed ligand complexes of Pd(II) and Cd(II) with N-picolyl-amine dithiocarbamate (PAC-dtc) as primary ligand and tertiary phosphine ligand as secondary ligands have been synthesized and characterized via elemental analysis, molar conductance, NMR (1H and 31P), and IR techniques. The PAC-dtc ligand displayed in a monodentate fashion via sulfur atom whereas diphosphine ligands coordinated as a bidentate mode to afford a square planner around the Pd(II) ion or tetrahedral around the Cd(II) ion. Except for complexes [Cd(PAC-dtc)2(dppe)] and [Cd(PAC-dtc)2(PPh3)2], the prepared complexes showed significant antimicrobial activity when evaluated against Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. Moreover, DFT calculations were performed to investigate three complexes {[Pd(PAC-dtc)2(dppe)](1), [Cd(PAC-dtc)2(dppe)](2), [Cd(PAC-dtc)2(PPh3)2](7)}, and their quantum parameters were evaluated using the Gaussian 09 program at the B3LYP/Lanl2dz theoretical level. The optimized structures of the three complexes were square planar and tetrahedral geometry. The calculated bond lengths and bond angles showed a slightly distorted tetrahedral geometry for [Cd(PAC-dtc)2(dppe)](2) compared to [Cd(PAC-dtc)2(PPh3)2](7) due to the ring constrain in the dppe ligand. Moreover, the [Pd(PAC-dtc)2(dppe)](1) complex showed higher stability compared to Cd(2) and Cd(7) complexes which can be attributed to the higher back-donation of Pd(1) complex.

In this study, chlorophenyltin(IV) [(C6H5)(Cl)Sn(L)2] and diphenyltin(IV) [(C6H5)2Sn(L)2] of N-methyl-N-hydroxyethyldithiocarbamate were prepared and characterized using various spectroscopic methods (FTIR, 1H, 13C, and 119Sn NMR) and elemental analysis. The FTIR and NMR spectral data, used to establish the structure of the compounds, showed the formation of the complexes via coordination to the two sulfur atoms from the dithiocarbamate ligand and the respective phenyltin(IV) derivatives. This coordination mode was further explored by DFT calculations, which showed that the bonding around the Sn center in [(C6H5)2Sn(L)2] was more asymmetric compared to the bonding around [(C6H5)(Cl)Sn(L)2]. However, the Sn–S bonds in [(C6H5)(Cl)Sn(L)2] were found to be more covalent than those in [(C6H5)2Sn(L)2]. Furthermore, the charge density of the frontier orbitals showed that the Sn atom in the complexes is relatively electrophilic and the Sn atom in [(C6H5)2Sn(L)2] has a lower atomic dipole moment than that of [(C6H5)(Cl)Sn(L)2]. The cytotoxicity and anti-inflammatory study revealed that [(C6H5)2Sn(L)2], with the higher number of phenyl substituents, has a higher potency than [(C6H5)(Cl)Sn(L)2]. The bio-efficacy study of these complexes as cytotoxic and anti-inflammatory agents showed that the complexes possessed moderate to high activity in comparison to the camptothecin and diclofenac in each case. Nevertheless, the diphenyltin(IV) derivative [(C6H5)2Sn(L)2] was found to possess a better activity than its counterpart due to the number of phenyl rings attached to the Sn center. [ABSTRACT FROM AUTHOR]