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We report our initial real-world experience with 177Lu-PSMA-617 radioligand therapy. Methods: We performed a retrospective review of patients treated with 177Lu-PSMA-617. Pretreatment PSMA PET, laboratory findings, overall survival, a fall in prostate-specific antigen by 50% (PSA50), and toxicities were evaluated. Results: Ninety-nine patients were included. Sixty patients achieved a PSA50. Seven of 18 (39%) patients who did not meet the TheraP PSMA imaging criteria achieved a PSA50. Nineteen of 31 (61%) patients who did not meet the VISION laboratory criteria achieved a PSA50. Sixty-three patients had a delay or stoppage in therapy, which was due to a good response in 19 patients and progressive disease in 14 patients. Of 10 patients with a good response who restarted treatment, 9 subsequently achieved a PSA50 on retreatment. The most common toxicities were anemia (33%) and thrombocytopenia (21%). Conclusion: At our center, patients who did not meet the TheraP PSMA imaging criteria or the VISION laboratory criteria benefited from 177Lu-PSMA-617 radioligand therapy.

BACKGROUND: We evaluated dolutegravir pharmacokinetics in infants with human immunodeficiency virus (HIV) receiving dolutegravir twice daily (BID) with rifampicin-based tuberculosis (TB) treatment compared with once daily (OD) without rifampicin. METHODS: Infants with HIV aged 1-12 months, weighing ≥3 kg, and receiving dolutegravir BID with rifampicin or OD without rifampicin were eligible. Six blood samples were taken over 12 (BID) or 24 hours (OD). Dolutegravir pharmacokinetic parameters, HIV viral load (VL) data, and adverse events (AEs) were reported. RESULTS: Twenty-seven of 30 enrolled infants had evaluable pharmacokinetic curves. The median (interquartile range) age was 7.1 months (6.1-9.9), weight was 6.3 kg (5.6-7.2), 21 (78%) received rifampicin, and 11 (41%) were female. Geometric mean ratios comparing dolutegravir BID with rifampicin versus OD without rifampicin were area under curve (AUC)0-24h 0.91 (95% confidence interval, .59-1.42), Ctrough 0.95 (0.57-1.59), Cmax 0.87 (0.57-1.33). One infant (5%) receiving rifampicin versus none without rifampicin had dolutegravir Ctrough

BACKGROUND: Dolutegravir (DTG) is a cornerstone of global antiretroviral (ARV) therapy (ART) due to its high efficacy and favorable tolerability. However, limited data exist regarding the risk of emergent integrase strand transfer inhibitor (INSTI) drug-resistance mutations (DRMs) in individuals receiving DTG-containing ART. METHODS: We performed a PubMed search using the term Dolutegravir, last updated 18 December 2023, to estimate the prevalence of VF with emergent INSTI DRMs in people living with HIV (PLWH) without previous VF on an INSTI who received DTG-containing ART. RESULTS: Of 2131 retrieved records, 43 clinical trials, 39 cohorts, and 6 cross-sectional studies provided data across 6 clinical scenarios based on ART history, virological status, and co-administered ARVs: (1) ART-naïve PLWH receiving DTG plus two NRTIs; (2) ART-naïve PLWH receiving DTG plus lamivudine; (3) ART-experienced PLWH with VF on a previous regimen receiving DTG plus two NRTIs; (4) ART-experienced PLWH with virological suppression receiving DTG plus two NRTIs; (5) ART-experienced PLWH with virological suppression receiving DTG and a second ARV; and (6) ART-experienced PLWH with virological suppression receiving DTG monotherapy. The median proportion of PLWH in clinical trials with emergent INSTI DRMs was 1.5% for scenario 3 and 3.4% for scenario 6. In the remaining four trial scenarios, VF prevalence with emergent INSTI DRMs was ≤0.1%. Data from cohort studies minimally influenced prevalence estimates from clinical trials, whereas cross-sectional studies yielded prevalence data lacking denominator details. CONCLUSIONS: In clinical trials, the prevalence of VF with emergent INSTI DRMs in PLWH receiving DTG-containing regimens has been low. Novel approaches are required to assess VF prevalence with emergent INSTI DRMs in PLWH receiving DTG in real-world settings.

A greener, safer, and more efficient methodology for the synthesis of (Z)‐5‐benzylidene‐2‐thioxothiazolidin‐4‐ones (3 a–u) and (Z)‐5‐benzylidenethiazolidine‐2,4‐diones (4 a–i) has been developed. The deep eutectic solvent (DES) ZnCl2/urea used as a greener solvent as well as a catalyst in this study accelerated the condensation of rhodanine and thiazolidine‐2,4‐dione with different aldehydes to afford the target scaffolds in excellent yields (88‐98 %). The reaction methodology adopted offered significant advantages such as mild reaction conditions, functional group tolerance, quick reaction time, column‐free isolation, catalytic recyclability, and applicability to gram‐scale production. Moreover, density function theory calculations were carried out to investigate the global reactivity and stability profiles of these compounds. Finally, the green metrics analysis supported the greener nature of the present methodology. [ABSTRACT FROM AUTHOR]

C(sp3)‐rich heterocycles are privileged building blocks for pharmaceuticals and agrochemicals. Therefore, synthetic methods that provide access to novel saturated nitrogen‐containing heterocycles are in high demand. Herein, we report a general synthesis of 1‐azabicyclo[2.1.1]hexanes (1‐aza‐BCH) via a formal cycloaddition of azabicyclo[1.1.0]butanes (ABB) with styrenes under photochemical conditions. To overcome the challenging direct single electron reduction of ABBs, we designed a polar‐radical‐polar relay strategy that leverages a fast acid‐mediated ring‐opening of ABBs to form bromoazetidines, which undergo efficient debrominative radical formation to initiate the cycloaddition reaction. The reaction is applicable to a broad range of ABB‐ketones and we demonstrate the 1‐aza‐BCH products can be further functionalized to access larger saturated, conformationally rigid heterocycles. [ABSTRACT FROM AUTHOR]

π-Stacking is common in materials, but different π–π stacking modes remarkably affect the properties and performances of materials. In particular, weak interactions, π-stacking and hydrogen bonding often have a significant impact on the stability and sensitivity of high-energetic compounds. A fused [5,7,5]-tricyclic energetic compound with a conjugated structure has been designed and synthesized. 4 H -[1,2,5]Oxadiazolo[3,4- e ][1,2,4]triazolo[3,4- g ][1,2,4]triazepin-8-amine is obtained in 48% yield from 3-amino-4-carboxy-1,2,5-oxadiazole through an efficient two-step reaction. Owing to its layered planar structure and weak π interactions between layers, 4 H -[1,2,5]oxadiazolo[3,4- e ][1,2,4]triazolo[3,4- g ][1,2,4]triazepin-8-amine exhibits high thermal stability (Td = 318 °C), low sensitivity (IS = 40 J, FS = 360 N), and relatively excellent detonation performance (D = 7059 ms–1 , P = 20.2 GPa). This detonation performance is superior to that of the conventional explosive TNT. The developed procedure provides a new method for the synthesis of fused ring compounds. [ABSTRACT FROM AUTHOR]

The present article presents a personal account on the synthesis of heterocycles by the combination of regioselective Pd-catalyzed cross-coupling reactions of polyhalogenated heterocycles, i.e., Suzuki–Miyaura and Sonogashira reactions, with alkyne-carbonyl-metathesis (ACM) reactions. The products, which show interesting optical, electronic or medicinal properties, are not readily available by other methods. [ABSTRACT FROM AUTHOR]

Introduction: The subarachnoid space in the brain contains crucial blood vessels and cerebrospinal fluid. Aneurysms in these vessels can lead to subarachnoid hemorrhage (SAH), a serious stroke subtype with high morbidity and mortality rates. SAH treatment includes procedures like coiling and clipping, but these are available only at comprehensive stroke centers (CSCs), necessitating urgent diagnosis and transfer to specialized facilities. Methods: This IRB-approved study was conducted by Polk County Fire Rescue (PCFR) in Florida. PCFR, serving an 850,000-person population, implemented a three-step SAH protocol. The protocol uses both Ottawa SAH criteria and recurring symptoms, such as new-onset seizures and high systolic blood pressure, that were identified by EMS. Acute management included administering labetalol, levetiracetam, and ondansetron. Results: Of 2175 stroke patients, 80 screened positive for SAH and were eligible for transfer. Patients had a median age of 66, and 33% had an initial systolic BP over 220 mmHg. The interfacility transfer rate dropped from 12.9 to 3.6% after implementing the protocol. Conclusion: The PCFR protocol's effectiveness suggests its potential for nationwide implementation. Early SAH recognition and prompt transfer to CSCs reduce complications and improve outcomes. Accurate field diagnosis by EMTs can prevent unnecessary transfers and enhance patient care. Future improvements may include portable diagnostic tools and enhanced EMT training to further improve SAH patients' pre-hospital care. [ABSTRACT FROM AUTHOR]

ABSTRACT A series of new 4a,7a‐diarylperhydroimidazo[4,5‐e][1,2,4]triazine‐3‐thiones were synthesized from 4,5‐diaryl‐4,5‐dihydroxyimidazolidin‐2‐ones and thiosemicarbazide in high yields, and their interaction with ethyl phenylpropiolate was studied. An effective method for the regioselective synthesis of imidazo[4,5‐e][1,3]thiazino[3,2‐b][1,2,4]triazines as new heterocycic system derivatives was proposed based on the reaction of aforementioned imidazotriazinethiones with ethyl phenylpropiolate in the presence of MeONa in methanol. The reaction is initiated by a Michael‐type addition of the imidazotriazinethiones to the triple bond of ethyl phenylpropiolate followed by intramolecular cyclization. [ABSTRACT FROM AUTHOR]

The green synthesis of medicines with an indazole skeleton has gained significant attention in recent years. Sustainable and environmentally friendly approaches for the synthesis of this important class of heterocyclic compounds from azobenzenes are attractive but rare. In this work, a series of neat, fast, and efficient reactions are well developed as a notable methodology for the photo-organic synthesis of indazoles. Metal and hydrogen source-free direct deoxygenative cyclization of o-carbonyl azobenzene under visible light is achieved through a new mechanism with huge potential in reduction cyclization reactions. Most examples are shown to give the corresponding 2H-indazole products in excellent yields, demonstrating that the present reaction has a wide substrate scope and good functional group tolerance. [ABSTRACT FROM AUTHOR]

As a result of its high reactivity, furan-2(3H)-one derivative 2 can be selected as a versatile and suitable candidate for building of novel nitrogen heterocyclic compounds. Consequently, furan-2(3H)-one derivative 2 and some nitrogen nucleophiles were utilized as starting materials for the formation of new pyridazinone and pyrrolone derivatives bearing naphthalene moiety. The continuous buildup of insecticide resistance is the main obstacle facing pest control measures. Pyrrole-based insecticides are a favourable choice due to their unique mode of action and no cross-resistance with traditional neurotoxic insecticides. The larvicidal activities of pyrrolone derivatives were assessed against field and laboratory strains of Culex pipiens larvae in comparison with chlorfenapyr (pyrrole insecticide). Compounds 17 (21.05 µg/mL) > 9 (22.81 µg/mL) > 15 (24.39 µg/mL) > 10 (26.76 µg/mL) > 16 (32.09 µg/mL) were most effective against lab strain of C. pipiens larvae relative to chlorfenapyr (25.43 µg/mL). While in field strain, 17 and 15 were the most toxic compounds followed by 9 > 10 > 16 > 2 with LC50 of 9.87, 10.76, 11.52, 12.68, 15.32 and 18.37 µg/mL, respectively, compared with chlorfenapyr with 14.03 µg/mL. The cytochrome P-450 monooxygenase activities were significantly increased in treated larvae of lab and field strains relative to untreated. The great variations in toxicity of the synthesized compounds were interpreted by structure-activity relationship study. The pyrrolone derivatives are effective against field and insecticide-resistant strains. Therefore, they are considered promising compounds to be integrated into pest management programs. [ABSTRACT FROM AUTHOR]

AbstractImidazole, a five-membered heterocyclic compound, has multipurpose applications for its bioactivity, uses in charge transport materials, and NLO materials. The review provides a comprehensive survey of the synthetic strategies of imidazole from various starting materials, highlighting their percentage yield and mechanistic insights. The most popular starting materials for the syntheses of imidazole include diketones, cyanides, imines, amidines, imidamides, di-amines, and oximes. Although the selection of a particular synthetic strategy will depend largely on the desired imidazole derivative, the survey consists of more than a century of research on imidazole synthetic procedures, starting with Heinrich Debus synthesis in 1858 till the present day. Most recent advancements and future perspectives in the field have been explored. The study will help researchers choose the most suitable starting material, catalyst, solvent, or reaction conditions for the synthesis of various imidazole derivatives. [ABSTRACT FROM AUTHOR]

Calix[n]porphyrinoids containing both sp2 and sp3meso‐carbons can bind metals like porphyrinoids and anions like calix[n]pyrroles. Thus, calix[n]porphyrinoids are hybrid macrocycles of porphyrinoids and calix[n]pyrroles. The core‐modified calix[n]porphyrinoids resulted by replacing one or more pyrroles of calix[n]porphyrinoids with different heterocycles or carbacycles that possesses very attractive structural, spectral, and coordination properties. For the past two decades, several different types of core‐modified calix[n]porphyrinoids in which one or more pyrroles were replaced with other heterocycles such as thiophene, selenophene, tellurophene, silole, phosphole, pyridine, etc and carbacycles such as m/p‐phenylene have been synthesized and explored their structure, metal coordination and anion sensing properties. This review describes different synthetic strategies used for the synthesis of various types of core‐modified calix[4]phyrins and expanded calix[n]phyrins and discusses their key structural aspects, properties, coordination chemistry and applications. [ABSTRACT FROM AUTHOR]

Background In 2019, the World Health Organization called for operational research on all-oral shortened regimens for multidrug- and rifampicin-resistant tuberculosis (MDR/RR-TB). We report safety and effectiveness of three 9-month all-oral regimens containing bedaquiline (Bdq), linezolid (Lzd), and levofloxacin (Lfx) and reinforced with cycloserine (Cs) and clofazimine (Cfz), delamanid (Dlm) and pyrazinamide (Z), or Dlm and Cfz. Methods We conducted a prospective cohort study of patients initiating treatment for pulmonary MDR/RR-TB under operational research conditions at public health facilities in Kazakhstan. Participants were screened monthly for adverse events. Participants with baseline resistance were excluded from the study and treated with a longer regimen. We analyzed clinically relevant adverse events of special interest in all participants and sputum culture conversion and end-of-treatment outcomes among individuals who were not excluded. Results Of 510 participants, 41% were women, the median age was 37 years (25th–75th percentile: 28–49), 18% had a body mass index <18.5 kg/m2, and 51% had cavitary disease. A total of 399 (78%) initiated Bdq-Lzd-Lfx-Cs-Cfz, 83 (16%) started Bdq-Lzd-Lfx-Dlm-Z, and 28 (5%) initiated Bdq-Lzd-Lfx-Dlm-Cfz. Fifty-eight individuals (11%) were excluded from the study, most commonly due to identification of baseline drug resistance (n = 52; 90%). Among the remaining 452 participants, treatment success frequencies were 92% (95% CI: 89–95%), 89% (95% CI: 80–94%), and 100% (95% CI: 86–100%) for regimens with Cs/Cfz, Dlm/Z, and Dlm/Cfz, respectively. Clinically relevant adverse events of special interest were uncommon. Conclusions All regimens demonstrated excellent safety and effectiveness, expanding the potential treatment options for patients, providers, and programs. [ABSTRACT FROM AUTHOR]

Introduction of non‐hexagons and/or heteroatoms allows for finely tuning the physicochemical properties of nanographenes. Heteroatoms doping have dominated the modulation of nanographenes with tunable band gap, rich electrochemical activities and so on. The pair of non‐hexagons, for instance, pentagon‐heptagon pairs, have furnished nanographenes with aromatic and/or antiaromatic characteristics, open‐shell properties and so on. In order to meet the growing demand for versatile nanographenes in materials science, research on novel nanographenes with heteroatom doped non‐hexagonal pairs has been aroused in recent years. In this review, we focus on nanographenes with nitrogen‐doped non‐hexagonal paris including the synthesis, structure analysis, photophysical properties, and potential applications in organic devices. [ABSTRACT FROM AUTHOR]

Trifluoromethyl heterocyclic compounds have high lipophilicity, metabolic stability and binding selectivity, so it is very important to develop their synthetic methods. This review provides an overview of synthesis of trifluoromethyl substituted heterocyclic compounds from β-trifluoromethylated acrylates over the period from 2018 to the present. [ABSTRACT FROM AUTHOR]

Herein we report a new, practical and efficient preparation of benzofuran-3-carboxylates and naphthofuran-3-carboxylates starting from β-nitroacrylates and phenols. The reaction is promoted by indium trichloride and leads to the target compounds in good to very good yields under microwave irradiation. [ABSTRACT FROM AUTHOR]

Breaking aromaticity by inserting additional atoms within the skeleton of heteroaromatic rings has gained significant attention over the years. As part of the emerging concept of 'skeletal editing', this short review retraces the recent progress made on dearomative enlargement reactions of both five- and six-membered heterocycles. 1 Introduction 2 Dearomative Enlargement of Five-Membered Rings 2.1 Pyrroles, Furans, Thiophenes and Their Fused Analogues 2.2 Pyrazoles, Isoxazoles, Isothiazoles and Their Fused Analogues 3 Dearomative Enlargement of Six-Membered Rings 4 Conclusion and Perspectives [ABSTRACT FROM AUTHOR]

The medicinal importance, natural rarity, and challenges associated with the synthesis of C3-functionalized 1 H -indazoles have propelled the development of novel and practical 1 H -indazole N-oxides for the production of diverse arrays of C3-functionalized 1 H -indazoles. The use of 1 H -indazole N-oxides has been remarkably effective for the selective introduction of diverse functional groups, including amino (NHAr), chloro (Cl), hydroxy (OH), sulfonyl (SO2 Ar), aromatic (Ar), olefin, alkyl, and N-formyl (NRCHO) groups, to indazole pharmacophore molecules. This review offers a concise overview of the synthetic approaches and practical applications of 1 H -indazole N-oxides, including recent studies conducted by the authors. Transformative reactions involving 1 H -indazole N-oxides not only offer strategies for synthesizing C3-functionalized 1 H -indazoles but also hold significant potential in medicinal chemistry. 1 Introduction 2 Synthetic Approaches and Applications of 1 H -Indazole N -Oxides 3 Summary and Outlook [ABSTRACT FROM AUTHOR]

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Background: Neuroinflammation is widely recognized as a key factor in the pathogenesis of Alzheimer's disease (AD), alongside ß-amyloid deposition and the formation of neurofibrillary tangles. The NLR family pyrin domain containing 3 (NLRP3) inflammasome, part of the innate immune system, has been implicated in the neuropathology of both preclinical amyloid and tau transgenic models. Activation of the NLRP3 pathway involves an initial priming step, which increases the expression of Nlrp3 and interleukin (IL)-1ß, followed by the assembly of the NLRP3 inflammasome complex, comprising NLRP3, ASC, and caspase-1. This assembly leads to the proteolytic maturation of the pro-inflammatory cytokines IL-1ß and IL-18. Additionally, the NLRP3 inflammasome induces Gasdermin D (GSDMD) cleavage, forming membrane pores through which IL-1ß and IL-18 are secreted. Inhibition of NLRP3 has been shown to enhance plaque clearance by modulating microglial activation. Furthermore, blocking NLRP3 in tau transgenic mice has been found to reduce tau phosphorylation by affecting the activity of certain tau kinases and phosphatases. Methods: In this study, organotypic brain slice cultures from P301S transgenic mice were treated with lipopolysaccharide (LPS) plus nigericin as a positive control or exposed to tau seeds (K18) to evaluate NLRP3 inflammasome activation. The effect of tau seeding on NLRP3 activity was further examined using Meso Scale Discovery (MSD) assays to measure IL1ß secretion levels in the presence and absence of NLRP3 inhibitors. The role of NLRP3 activity was investigated in fullbody Nlrp3 knockout mice crossbred with the tau transgenic P301S model. Additionally, full-body and microglia-selective Gsdmd knockout mice were crossbred with P301S mice, and tau pathology and neurodegeneration were evaluated at early and late stages of the disease using immunohistochemistry and biochemical assays. Results: Activation of the NLRP3 pathway was observed in the mouse organotypic slice culture (OSC) model following stimulation with LPS and nigericin or exposure to tau seeds. However, Nlrp3 deficiency did not mitigate tauopathy or neurodegeneration in P301S mice in vivo, showing only a minor effect on plasma neurofilament (NF-L) levels. Consistently, Gsdmd deficiency did not alter tau pathology in P301S mice. Furthermore, neither full-body nor microglia-selective Gsdmd deletion had an impact on neuronal pathology or the release of pro-inflammatory cytokines. Conclusion: The absence of key components of the NLRP3 inflammasome pathway did not yield a beneficial effect on tau pathology or neurodegeneration in the preclinical Tau-P301S mouse model of AD. Nonetheless, organotypic slice cultures could serve as a valuable ex vivo mechanistic model for evaluating NLRP3 pathway activation and pharmacological inhibitors. [ABSTRACT FROM AUTHOR]

Objective: Given the lack of global consensus on anesthesia selection for peritoneal dialysis catheter (PDC) placement via open surgery, this study investigates the safety and efficacy of combining local infiltration anesthesia (LIA) with monitored anesthesia care (MAC) in patients with end-stage renal disease (ESRD). Methods: This retrospective analysis of ESRD patients who underwent open surgical placement of PDC in the Department of Nephrology, the First Affiliated Hospital of the Army Medical University from 1 August 2020 to 31 May 2022. Patients were categorized into two groups based on anesthesia method: LIA group and LIA + MA group. MA was defined as preoperative sedation (0.2–0.7 µg/kg/h) with dexmedetomidine injection (Huidrican trade name, DEX), and intraoperative analgesia with dexrazoxane injection (Garonin trade name, DEZ) as appropriate according to the patients' pain scores. We compared the general clinical data of the two groups of patients, the changes in blood pressure and heart rate during the whole operation, the intraoperative and postoperative pain, the total duration of the operation and the immediate postoperative complications. Results: The study included 123 patients (59 in the LIA + MAC group and 64 in the LIA group). The LIA + MA group exhibited lower pain scores measured by Visual Analogue Scale(VAS) during surgery (skin incision, subcutaneous adipose tissue dissection, anterior fascia, muscle traction, posterior fascia, peritoneum, and catheterization) compared to the LIA group(p<0.05). In terms of surgical incisions, to intraoperative pain scores (VRS), the LIA + MA group showed higher score level I and lower score level II compared to the LIA group (p = 0.002, 0.004, respectively). The LIA + MA group experienced lower postoperative resting pain (NRS) and VAS than the LIA group (p = 0.001,0.003, respectively). The surgical duration for the LIA + MA group was shorter than that of the LIA group (p<0.001). Preoperative systolic and diastolic blood pressures (SBP and DBP) were higher in the LIA + MA group compared to the LIA group (p<0.001,<0.001, respectively). Postoperative heart rate and DBP were lower in the LIA + MA group (p<0.001, 0.004, respectively). The LIA + MA group exhibited greater changes in heart rate, SBP, and DBP during and after surgery compared to the LIA group (p = 0.009, <0.001,<0.001, respectively). In terms of immediate postoperative complications, the proportion of patients requiring analgesics within 24 h post-surgery was significantly lower in the LIA + MA group (p = 0.031). Conclusion: Open surgery for PDC placement under LIA + MAC is both safe and effective. The key points: There is no global consensus on the preferred anesthesia method for PDC placement. DEX combined with analgesics may yield synergistic effects and serve as a backup rescue analgesic. PDC placement under LIA + MA is safety and efficacy. [ABSTRACT FROM AUTHOR]

ABSTRACT Many molecules called coumarins with very varied biological activities and widely used in the food, pharmaceutical, cosmetic, and medical industries. Their structure has a significant impact on their biological activity and their possible applications. Advanced synthesis frequently leads to an increase in the production of various chemical wastes. The amount of hazardous organic substances used and produced is reduced by the application of environmentally friendly synthesis techniques. Numerous techniques are employed in green chemistry, including the use of ionic liquids and deep eutectic solvents, solvent‐free synthesis, mechanical synthesis, multicomponent reactions, ultrasound, and microwaves. These green synthesis techniques have been successfully applied to all common condensation reactions for the synthesis of coumarin, including the Perkin, Knoevenagel, Pechmann, Kostanecki‐Robinson, and Reformansky reactions. These methods not only reduce the use and production of toxic chemicals, but also improve the yield, purity, and energy consumption of the product. This review summarizes the methods of microwave synthesis of coumarin derivatives, as well as their biological activities. [ABSTRACT FROM AUTHOR]

AbstractThe Pummerer rearrangement is extensively utilized for the preparation of various heterocyclic compounds, as well as for the introduction of functional groups such as carbonyl, hydroxyl, and amino groups into organic molecules. The reaction mechanism typically proceeds through an initial electrophilic attack by Lewis acid or another electrophile on the sulfur atom of the sulfoxide, leading to the formation of a sulfonium intermediate. Subsequent rearrangement of this intermediate results in the migration of an alkyl/aryl group from sulfur to a neighboring carbon atom, accompanied by the expulsion of a leaving group. The Pummerer rearrangement of quinoline derivatives has significant synthetic utility and has been employed in the synthesis of various compounds. It has found applications in the synthesis of natural products, agrochemicals, pharmaceuticals, diversity-oriented synthesis, functional group transformations, and other fine chemicals. Overall, The Pummerer rearrangement of quinoline derivatives offers a versatile tool for the synthesis of complex molecules in medicinal chemistry. [ABSTRACT FROM AUTHOR]

Chiral N‐heterocyclic compounds are key structures in natural compounds and pharmaceuticals, and they serve as essential building blocks of functional materials. Catalytic asymmetric cycloaddition reactions represent one of the most efficient synthetic strategies for constructing optically active heterocycles. Cyclic sulfamidate imines have recently come to be extensively studied and widely utilized in both organocatalytic and transition metal‐catalyzed asymmetric cycloadditions, where they have been shown to provide various N‐fused‐heterocycles and spiro‐cycles exhibiting high efficiencies with excellent stereoselectivities. This review highlights recent advancements in catalytic asymmetric cycloadditions of cyclic sulfamidate imines for the stereoselective synthesis of biologically active sulfamidate‐containing heterocycles since 2012 while focusing on the diverse reactivities of cyclic sulfamidate imines and the mechanisms of chiral induction in catalysis. [ABSTRACT FROM AUTHOR]

AbstractIn recent years, the inadequacy and high costs of current cancer treatment drugs have led to an increase in research focused on the design and synthesis of new compounds with potential applications in this field and the evaluation of their anticancer properties using in silico methods. For this purpose, four novel heterocyclic compounds (6–9) were synthesized and characterized using spectroscopic techniques. The DFT approach and B3LYP/6-311G(d,p) basis set were used to compare theoretical data with experimental ones and to obtain optimized geometries. It was observed that experimental and theoretical data were in harmony. In silico techniques were used to investigate the potential of synthesized compounds as drug candidates. ADMEt results have shown that all synthesized compounds have Lipinski’s rule of five which has searched criteria in drug candidates. Molecular docking studies were also performed against cancer-related proteins. The highest docking score between 2XIR protein and compound 8 was found to be −11.7 kcal/mol, while the lowest was −8.2 kcal/mol between 1MP8 protein and compound 9. To do meaningful comparisons standard drugs were also used in Molecular Docking studies. It was observed that all synthesized molecules had higher docking scores than standard drugs except ifebemtinib. It can be suggested that based on ADMET and molecular docking studies compound 8 has the potential to be a drug candidate after further investigations such as in vitro, in silico, etc., have been performed in this area. [ABSTRACT FROM AUTHOR]

N‐heterocyclic compounds have a broad range of applications and their selective synthesis is very appealing for the pharmaceutical and agrochemical industries. Herein we report the usage of the flavin‐dependent nitroreductase BaNTR1 for the photoenzymatic synthesis of various anthranils and quinolines from retro‐synthetically designed o‐nitrophenyl‐substituted carbonyl substrates, achieving high conversions (up to >99 %) and good product yields (up to 96 %). Whereas the effective production of anthranils required the inclusion of H2O2 in the reaction mixtures to accumulate the needed hydroxylamine intermediates, the formation of quinolines required the use of anaerobic or reducing conditions to efficiently generate the essential amine intermediates. Critical to our success was the high chemoselectivity of BaNTR1, performing selective reduction of the nitro group without reduction of the carbonyl moiety or the activated carbon‐carbon double bond. The results highlight the usefulness of an innocuous chlorophyll‐ and nitroreductase‐based photoenzymatic system for the tailored synthesis of diverse N‐heterocycles from simple nitro compounds. [ABSTRACT FROM AUTHOR]

Hypervalent iodine reagents are versatile and readily accessible reagents that have been extensively applied in contemporary synthesis in modern organic chemistry. Among them, iodonitrene (ArI=NR), is a powerful reactive species, widely used for a single‐nitrogen‐atom insertion reaction, and skeletal editing to construct N‐heterocycles. Skeletal editing with reactive iodonitrene components has recently emerged as an exciting approach in modern chemical transformation. These reagents have been extensively used to produce biologically relevant heterocycles and functionalized molecular architectures. Recently, the insertion of a nitrogen‐atom into hydrocarbons to generate N‐heterocyclic compounds using hypervalent iodine reagents has been a significant focus in the field of molecular editing reactions. In this review, we discuss the rapidly emerging field of nitrene insertion, including skeletal editing and nitrogen insertion, using hypervalent iodine reagents to access nitrogen‐containing heterocycles, and the current mechanistic understanding of these processes. [ABSTRACT FROM AUTHOR]

There is a significant amount of research being conducted in the field of nitrogen-containing heterocycles due to their diverse applications in different industries. Benzimidazole is one of the heterocyclic compounds formed by connecting the benzene and imidazole rings and shows diverse biological activities. Benzimidazole is also an essential compound in agriculture and industry. In this research, the NiFe2O4@SiO2-Pr-S-nBu-SO3H nanocomposite was prepared and used as a heterogeneous catalyst for synthesizing the 2-aryl benzimidazole derivatives. This protocol involved the reaction between orthophenylene diamine and aromatic aldehydes, with iodine as an oxidizing agent. The prepared catalyst was thoroughly examined using various methods, including infrared Fourier transform spectroscopy (FT-IR), X-ray diffraction (XRD), scanning electron microscopy (SEM), vibrating sample magnetometry (VSM), and energy dispersive X-ray (EDX) spectroscopy. This protocol offers several advantages such as a short reaction time at room temperature, simple workup, high product yields, simple purification, availability of raw materials, and a catalyst that is both reusable and environmentally friendly. Finally, to characterize the organic compounds, the melting point, FT-IR, and 1H NMR analyses were utilized. [ABSTRACT FROM AUTHOR]

Upon reaction with α,β‐unsaturated nitriles (2 a–d) and/or salicylaldehyde, 3‐(naphthalen‐2‐yl)‐3‐oxopropanenitrile (1) yields pyridine derivatives 3 a–d and/or the imino chromene derivative 4. Compound 1 reacted with phenyl isothiocyanate in a basic medium to give the intermediate potassium salt 6. Upon stirring at room temperature, the intermediate 6 with some α‐halogenated compounds yielded the acyclic compounds 7, 9, 11, 13, and 15. On the other hand, refluxing intermediate 6 with the same α‐halogenated compounds in DMF in the presence of TEA afforded the corresponding thiophene derivatives 8, 10, 12, 14, and 16. The reaction of thiol 17 with hydrazine hydrate derivatives 18 a–d yielded the corresponding pyrazole derivatives 21 a–d. Compound 20 reacted with o‐phenylenediamine or o‐aminothiophenol in the presence of DMF/TEA to give the corresponding benzothiazole or benzoimidazole derivatives 27 a and 27 b, respectively. Thirty new synthesized compounds were examined for their antibacterial activity against Gram‐positive bacteria including S. aureus and B. subtilis, Gram‐negative bacteria such as P. aeruginosa and E. coli, and yeast‐like fungi like C. albicans in vitro. Compounds 15, 16, 21 d, 27 a, 27 b, exhibited the highest antibacterial activity against Gram‐positive bacteria. Molecular docking experiments were conducted to explore the binding affinities and interaction modalities of selected derivatives with the target PDB‐3cmt protein. [ABSTRACT FROM AUTHOR]

Piperazine, a nitrogen‐containing heterocyclic compound, has potential in medical chemistry due to its versatile structure and ease of modification. Therefore, researchers have designed novel piperazine derivatives with various biological activities, including antiviral, antibacterial, and antifungal properties. In this study, a new series of 2‐(4‐((5‐bromo‐2‐methoxyphenyl)sulfonyl) piperazine‐1‐yl) acetamide derivatives (7a‐l) were synthesized and their structures were identified using 1H‐NMR, 13C‐NMR, and HRMS spectroscopic methods. The in vitro antimicrobial activity of these compounds was tested against four bacterial strains and two fungi strains. Some of the sulfonyl piperazine derivatives (7d, 7e, 7f, 7j, 7k, and 7l) exhibited relatively good antimicrobial and antifungal activities compared to standard drugs. Further analysis using computational docking confirmed strong binding interactions, aligning with our results. Our compounds exhibited improved potency compared to existing standard treatments. [ABSTRACT FROM AUTHOR]

The identity of a heteroatom within an aromatic ring influences the chemical properties of that heterocyclic compound. Systematically evaluating the effect of a single atom, however, poses synthetic challenges, primarily as a result of thermodynamic mismatches in atomic exchange processes. We present a photocatalytic strategy that swaps an oxygen atom of furan with a nitrogen group, directly converting the furan into a pyrrole analog in a single intermolecular reaction. High compatibility was observed with various furan derivatives and nitrogen nucleophiles commonly used in drug discovery, and the late-stage functionalization furnished otherwise difficult-to-access pyrroles from naturally occurring furans of high molecular complexity. Mechanistic analysis suggested that polarity inversion through single electron transfer initiates the redox-neutral atom exchange processes at room temperature. [ABSTRACT FROM AUTHOR]

Introduction: The subarachnoid space in the brain contains crucial blood vessels and cerebrospinal fluid. Aneurysms in these vessels can lead to subarachnoid hemorrhage (SAH), a serious stroke subtype with high morbidity and mortality rates. SAH treatment includes procedures like coiling and clipping, but these are available only at comprehensive stroke centers (CSCs), necessitating urgent diagnosis and transfer to specialized facilities. Methods: This IRB-approved study was conducted by Polk County Fire Rescue (PCFR) in Florida. PCFR, serving an 850,000-person population, implemented a three-step SAH protocol. The protocol uses both Ottawa SAH criteria and recurring symptoms, such as new-onset seizures and high systolic blood pressure, that were identified by EMS. Acute management included administering labetalol, levetiracetam, and ondansetron. Results: Of 2175 stroke patients, 80 screened positive for SAH and were eligible for transfer. Patients had a median age of 66, and 33% had an initial systolic BP over 220 mmHg. The interfacility transfer rate dropped from 12.9 to 3.6% after implementing the protocol. Conclusion: The PCFR protocol's effectiveness suggests its potential for nationwide implementation. Early SAH recognition and prompt transfer to CSCs reduce complications and improve outcomes. Accurate field diagnosis by EMTs can prevent unnecessary transfers and enhance patient care. Future improvements may include portable diagnostic tools and enhanced EMT training to further improve SAH patients' pre-hospital care. [ABSTRACT FROM AUTHOR]

Polycyclic heterocycles are the most common and critical structural motifs found in a variety of natural products, medicines, fertilizers, and advanced materials. Because of their widespread use in biologically active compounds and material chemistry, functionalised dibenzo heterocyclic compounds, especially dibenzofuran, dibenzothiophene, and carbazole derivatives, garnered much attention over time. Scientists are especially interested in elucidating more efficient techniques for developing these industrially essential compounds. Dibenzo‐fused heterocycles can rapidly be synthesised using highly efficient transition metal‐catalysed strategies as well as by economic metal‐free reaction conditions. This review includes a detailed overview of the most recent significant synthetic techniques, both metal‐catalysed and metal‐free, to produce these industrially significant and medicinally important dibenzo‐fused heterocycles. [ABSTRACT FROM AUTHOR]

Olanzapine can have a better impact on negative symptoms of schizophrenia with reduced motor side effects compared to other atypical antipsychotics, according to some literature. Here, the authors describe a case of a woman with a diagnosis of schizophrenia who developed the rare side effect of bilateral pedal oedema while on oral olanzapine. The possible mechanism behind the condition and the clinical management measures taken to resolve the oedema is discussed. [ABSTRACT FROM AUTHOR]

Naphthylimides play a pivotal role as aromatic heterocyclic compounds, serving as the foundational structures for numerous pharmacologically significant drugs. These drugs encompass antibacterial, antifungal, anticancer, antimalarial, antiviral, anti-inflammatory, antithrombotic, and antiprotozoal agents. The planar and heteroaromatic characteristics of naphthylimides grant them a strong ability to intercalate into DNA. This intercalation property renders naphthylimide derivatives highly valuable for various biological activities. The advantageous pharmacological activity and ease of synthesis associated with naphthylimides and their derivatives provide significant benefits in the design and development of new compounds within this class. Currently, only a few such molecules are undergoing preclinical and clinical evaluations. In this paper, we have compiled the literature on naphthylimides reported by researchers from 2006 to 2024. Our focus lies on exploring the pharmacological activities of their analogues from a drug development and discovery perspective, while examining their structure–activity relationship and mechanisms of action. [ABSTRACT FROM AUTHOR]

Carbazole is an aromatic heterocyclic organic compound consisting of two fused benzene rings and a pyrrole ring and is a very valuable building structure for the design of many compounds for use in various fields of chemistry and medicine. This study presents three new carbazole-based thiazole derivatives that differ in the presence of a different halogen atom: chlorine, bromine, and fluorine. Experimental studies and quantum-chemical simulations show the effect of changing a halogen atom on the physicochemical, biological, and linear and nonlinear optical properties. We have also found that carbazoles C-Cl, C-Br, and C-F exhibit high tyrosinase inhibitory activity, with IC50 values in the range of 68–105 µM with mixed mechanism of action. Finally, molecular docking to the active site of Concanavalin A (ConA) and bioavailability for all compounds were evaluated. [ABSTRACT FROM AUTHOR]

Simple Summary: A review of the latest research at PubMed and major cancer conferences was conducted to find out the current treatments for advanced stomach and esophagogastric junction cancers. In the West, neoadjuvant and perioperative chemotherapy is preferred for localized tumors. In East Asia, adjuvant chemotherapy is preferred. Studies are looking at how well immunotherapy and other drugs work in the perioperative setting. To choose the best treatment for advanced gastric cancer, including adenocarcinoma of the esophago-gastric junction, it is important to know biomarkers like HER2 expression, PD-L1 combined positive score (CPS), Claudin 18.2, and microsatellite instability (MSI). The standard first-line therapy is a combination of fluoropyrimidine and a platinum derivative. The choice of chemotherapy with antibodies depends on the biomarker. This article reviews recent clinical trial results and looks at the future of systemic therapy. Background: The prognosis of patients diagnosed with locally advanced and metastatic gastric and esophago-gastric junction cancer is critical. The optimal choice of systemic therapy is essential to optimize survival outcomes. Methods: A comprehensive literature review via PubMed and analysis of major oncology congresses (European Society for Medical Oncology and American Society of Clinical Oncology websites) were conducted to ascertain the current status and latest developments in the systemic treatment of patients with localized or advanced gastric and esophago-gastric junction adenocarcinoma. Results: While neoadjuvant and perioperative chemotherapy for localized tumor stages is the preferred approach in the Western Hemisphere, adjuvant chemotherapy remains the preferred course of action in East Asia. The administration of chemotherapy, typically in the form of combinations comprising platinum and fluoropyrimidine compounds in combination with docetaxel, represents a standard of care. Investigations are underway into the potential of immunotherapy and other biologically targeted agents in the perioperative setting. To select the most appropriate therapy for advanced gastric cancer, including adenocarcinoma of the esophago-gastric junction, it is essential to determine biomarkers such as HER2 expression, PD-L1 combined positive score (CPS) (combined positive score), Claudin 18.2, and microsatellite instability (MSI). In the present clinical context, the standard first-line therapy is a combination of fluoropyrimidine and a platinum derivative. The selection of chemotherapy in combination with antibodies is contingent upon the specific biomarker under consideration. Conclusions: This article reviews the current state of the art based on recent clinical trial results and provides an outlook on the future of systemic therapy. [ABSTRACT FROM AUTHOR]

A KOtBu‐promoted robust strategy has been described for the regioselective synthesis of pyrrolo[3,4‐b]quinolin‐1‐one and naphthyridin‐1(2H)‐one derivatives from o‐alkynylquinolinecarbonitriles in good to excellent yields. The reaction proceeds through in situ transformation of the nitrile moiety into an amide group followed by the selective C−N bond formation through a 5‐exo‐dig or 6‐endo‐dig annulation reaction. Among the synthesized derivatives, 6‐endo‐dig naphthyridin‐1(2H)‐ones displayed good photophysical properties. The present approach is superior to other established methodologies as it avoids use of transition metals and column chromatographic purification and affords the products in high yields. Additionally, the current methodology provides several additional advantages, such as one‐pot operation, high atom economy, broad substrate scope and a step‐economical process. [ABSTRACT FROM AUTHOR]

ABSTRACT A method for efficient synthesis of quinolines via acceptorless dehydrogenative condensation is presented. A series of quinolines are obtained by the coupling reaction of 2‐aminobenzyl alcohols with secondary alcohols in the presence of bidentate terpyridine Mn(I) complex in good to excellent yields. Pleasantly, various substituted secondary alcohols and substituted aminobenzyl alcohols all provide quinolines with good functional group tolerance. Importantly, this investigation also provides a green and environmentally friendly protocol for constructing heterocyclic compounds. [ABSTRACT FROM AUTHOR]

The article focuses on an 8-year-old girl diagnosed with atypical hemolytic uremic syndrome (aHUS) after presenting with non-bloody diarrhea, hemolytic anemia, and thrombocytopenia. Topics include her clinical presentation with elevated blood pressure and kidney involvement, the negative tests for shiga toxin and the normal ADAMTS-13 activity, and her subsequent treatment with plasma exchange and eculizumab, leading to improved kidney function and the cessation of dialysis.

The article focuses on an 11-year-old boy presenting with slurred speech and involuntary movements, later diagnosed with a neurological disorder. Topics include his clinical symptoms such as dysarthria and abnormal involuntary movements, his physical exam findings including hyperreflexia and abnormal gait, and the absence of significant prior medical or family history.

Objectives: The aim of this study is to indirectly compare and rank the different drugs that have been studied in randomized clinical trials (RCTs) in patients with tardive dyskinesia (TD) in terms of their efficacy in ameliorating the symptoms of TD and safety. Design: A network meta-analysis and a systematic review were registered prospectively on PROSPERO under the ID: CRD42023407823 and were conducted in accordance with the PRISMA-NMA guidelines. Data sources: PubMed, Scopus, The Cochrane Central Register of Controlled Trials (CENTRAL), Web of Sciences, and Clinicaltrials.gov were searched to identify relevant records. Eligibility criteria for selecting studies: Any parallel randomized blinded controlled clinical trials that studied the use of any medications in treating TD and assessed the symptoms using a functional scale that has been previously validated. Data extraction: The standardized mean difference of improvement along with the reported adverse events for each drug was extracted from each trial, and a network meta-analysis was conducted using a random-effects model. Results: One thousand eight hundred seventeen patients in 33 RCTs were included in the analysis. Twenty-three different drugs were compared to placebo in terms of reduction in TD symptoms. Among these, valbenazine 80 mg (SMD = − 1.66, 95%CI = [− 2.55; − 0.78]), valbenazine 40 mg (− 1.00, [− 1.89; − 0.11]), and vitamin E (− 0.77, [− 1.45; − 0.1]) significantly reduced TD symptoms in comparison to placebo, while deutetrabenazine 36 mg (− 1.00, [− 2.12; 0.11]) and reserpine (− 0.54, [− 1.09; 0.02]) did not significantly reduce symptoms. Some serious adverse events were reported for valbenazine and deutetrabenazine, which included mainly psychiatric symptoms such as depression, worsening of schizophrenia, and suicidal ideation, while mild adverse events were reported for other drugs, and their incidence in the treatment arms was comparable to those in the placebo arm. Conclusions: Valbenazine (80 and 40 mg) and vitamin E demonstrated efficacy in treating tardive dyskinesia. However, the significant side effects of valbenazine should prompt further investigation of alternative treatment modalities. [ABSTRACT FROM AUTHOR]

The present article provides a personalized account on CH-arylation reactions employed for the synthesis of heterocycles. The presence of a nitro group allowed for direct and regioselective CH-arylations of pyrazoles, imidazoles, indoles and a variety of purine analogues. Direct CH-arylations without the presence of an activating nitro-group were employed for inter- and intramolecular reactions of purine derivatives, which allowed for the synthesis of a great variety of polycyclic systems. Domino C–N coupling / hydroamination / CH-activation reactions of diarylacetylenes with anilines allowed for the synthesis of polycondensated N -heterocycles. Products include indolo- and azaindolo[1,2- f ]phenanthridines, quinolino[3′,4′:4,5]pyrrolo[1,2- f ]phenanthridines, pyrimido[5′,4′:4,5]pyrrolo[1,2- f ]phenanthridines, and benzothieno[2′,3′:4,5]pyrrolo[1,2- f ]phenanthridines. The reaction of N -heterocycles, such as indoles, with 1,1-difluoroalkenes resulted in a twofold addition-elimination reaction to give 1,1-diaminoalkenes, which were transformed by CH-arylation into various polycondensated heterocycles, such as indoloisoquinolines, thienoindolizines, oxepines and helicenes. Pyridofluoranthenes, diindenopyrene and azadiindenopyrenes were prepared by a combination of Pd-catalyzed cross-coupling reactions with acid-mediated cycloisomerizations and Pd-catalyzed intramolecular CH-arylations. Bis(carbazoles), benzodithiazoles, benzodithiophenes and 2,5-diarylpyrroles were prepared by inter- and intramolecular CH-arylation reactions. [ABSTRACT FROM AUTHOR]

The dithioacetalization of lactaldehyde derivatives with ethane-1,2-, propane-1,3-, butane-1,4-, and pentane-1,5-dithiols in the presence of 4 mol% of scandium triflate has been described. A series of cyclic dithioacetals were obtained with yields ranging from quantitative to 37%. The dithioacetalization of lactaldehyde derivatives with butane-1,4-dithiol and pentane-1,5-dithiol groups are accompanied by the formation of 14- and 16-membered macrocyclic sulfur structures with yields of 3% and 18%, respectively. In the case of a cyclic dithioacetal derivative with three methylene groups, a diastereoisomeric pair of enantiomers was obtained, the structure of which was confirmed by single-crystal X-ray diffraction analysis. Dithioacetals are useful building blocks in the synthesis of complex chemical structures. Macrocyclic compounds can be used to complex metal ions. [ABSTRACT FROM AUTHOR]

The metal-free direct oxidative cross-dehydrogenative C–H bond amination of imidazopyridines with pyrazole in water as solvent has been developed under K2 S2 O8-promoted mild conditions. This strategy was applied to variable imidazoheterocycles to give amination products in moderate to good yields. The described protocol also offers scale-up synthesis for the construction of C–N bonds, which makes it suitable for the synthesis of biologically active compounds and pharmaceuticals. [ABSTRACT FROM AUTHOR]

Aminals, characterized by a central carbon linking two nitrogen atoms, are versatile building blocks in modern chemistry. This review addresses a literature gap by exploring the synthesis and applications of aminals, with a focus on drug discovery and molecular diversity. Beyond medicinal chemistry, aminals find applications as key components in bioactive compounds and as versatile tools in materials chemistry. The review covers fundamental characteristics, synthetic methodologies, stability, and applications, emphasizing alternative synthetic methods to the well-established aldehyde–amine condensation. This inclusive exploration provides insights into diverse synthetic pathways that expand the versatility of the aminal scaffold. 1 Introduction 2 The Aminal Group 3 Aminal Synthesis 3.1 Metal-Free Approaches 3.2 Metal-Catalyzed Approaches 3.3 Photoredox Methodologies 3.4 Via Rearrangements 3.5 Via Decarboxylative Coupling 4 Aminals as Synthetic Tools 5 Synthesis of Aminal-Containing Natural Products 6 Aminal-Based Materials 7 Conclusions [ABSTRACT FROM AUTHOR]

A phytochemical investigation on the 80% EtOH extract of the leaves of Paederia scandens (Lour.) Merr. resulted into the isolation of three undescribed iridoid glycosides, 10-O-trans-p-coumaroyl-(4R,6R)-3,4-dihydro-3α-methylthiopaederoside (1), 10-O-trans-feruloyl-(4S,6R)-3,4-dihydro-2′-O-3α-paederoside (2), and 10-O-trans-caffeoyl-paederosidic acid ethyl ester (3). The structures of the new compounds were elucidated by spectral methods such as 1D and 2D (1H-1H COSY, HMQC, and HMBC) NMR spectroscopy, as well as high resolution mass spectrometry. The isolated compounds were tested in vitro for cytotoxic activity against five endocrine tumor cell lines. As a result, compound 1 exhibited some cytotoxicities against all the tested tumor cell lines with IC50 value less than 20.0 μM. [ABSTRACT FROM AUTHOR]

Twenty 3-acyloxymaltol/ethyl maltol derivatives (7a-j and 8a-j) were synthesized and evaluated in vitro for their anti-oomycete activity against Phytophthora capsici, respectively. Among all of twenty derivatives, more than half of the compounds 7f, 7h, 8a-h and 8j had anti-oomycete activity higher than the positive control zoxamide (EC50 = 22.23 mg/L), and the EC50 values of 18.66, 20.32, 12.80, 16.18, 10.59, 14.98, 16.80, 10.36, 15.32, 12.64, and 13.59 mg/L, respectively. Especially, compounds 8c and 8f exhibited the best anti-oomycete activity against P. capsici with EC50 values of 10.59 and 10.36 mg/L, respectively. Overall, hydroxyl group of maltol/ethyl maltol is important active modification site. [ABSTRACT FROM AUTHOR]

Dinitropyridines are one of the promising classes of heterocyclic compounds. They are considered as useful precursors of explosives and energetic compounds, agrochemicals, biosensors and biologically active compounds with diverse properties: antitumor, antiviral, anti‐neurodegenerative. Preliminary analysis of literature data shows that the chemistry of polynitropyridines has been actively developing over the past few decades. This is evidenced by the steadily growing annual number of publications. In this review the literature on the synthesis, reactions and practical application of isomeric dinitropyridines over a period of 2010–2024 is analyzed. [ABSTRACT FROM AUTHOR]