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Hydrogenation plays an important role in the production of bulk and fine chemicals. In the present work, the hydrogenation process of 1-cyanocyclohexaneacetic acid (1-CA), a key intermediate in the chemo-enzymatic synthesis of the antiepileptic drug gabapentin, was investigated. The catalysts were screened, the operating parameters for the 1-CA hydrogenation were determined by response surface methodology, and the effects of biological impurities on the reaction and catalysts were investigated. The reaction temperature, reaction solution pH and reaction time were identified as the main factors for hydrogenation by single-factor experiments. Under the optimal reaction conditions: reaction temperature 110 °C, solution pH 12.33, reaction time 3.74 h, hydrogen pressure 2 MPa and stirring speed 500 rpm, the substrate conversion reached 100%, and the total product yield reached 96.40%, which was very close to the prediction (96.88%). It was demonstrated that biological impurities greatly affect the reaction rate of hydrogenation, as well as the activity and reusability of the catalyst, in which protein impurities lead to catalyst deactivation through cumulative deposition on the catalyst surface and within the pores. [ABSTRACT FROM AUTHOR]

Objective: The aims of this article are to review the clinical aspects of rozanolixizumab, to describe clinical trial results that led to the drug's approval, and to examine the impact on patient care to aid clinical decision making. Data Sources: A PubMed search was conducted using the terms Rystiggo ™, rozanolixizumab, rozanolixizumab therapy, and myasthenia gravis. The most recent prescribing information was also used for information relating to the drug and for identification of pertinent studies. Study Selection/Data Extraction: Phase I, II, and III randomized controlled trials were all eligible for inclusion. Meeting abstracts and articles focusing on the use of rozanolixizumab or any indication other than generalized myasthenia gravis were excluded from this article. Data Synthesis: Food and Drug Administration approval of rozanolixizumab is based on the phase III MycarinG study in patients with generalized myasthenia gravis. A phase II trial explored initial clinical efficacy and safety pertaining to the dose and frequency of rozanolixizumab across 2 treatment periods in patients with moderate to severe myasthenia gravis. Relevance to Patient Care and Clinical Practice in Comparison to Existing Agents: Rozanolixizumab is the first therapy approved to treat patients positive for both types of antibodies, anti-acetylcholine receptor or anti-muscle-specific tyrosine kinase, in generalized myasthenia gravis. Conclusion/Relevance: The approval of rozanolixizumab represents an advancement in therapy for generalized myasthenia gravis. The provision of individualized, targeted, and well-tolerated treatment is valuable for the patients whose myasthenia gravis is not well controlled and who are seeking a medication with a rapid onset of action to improve their symptoms and overall quality of life. [ABSTRACT FROM AUTHOR]

The efficient preparation of long-chain amines via a one-step transfer-hydrogenation/reductive-amination reaction (THRA) of polyenals has been achieved. This strategy, which combines transfer hydrogenation and reductive amination, significantly enhances the synthetic efficiency of amino compounds. Additionally, this protocol offers a practical method for carbon-chain elongation/amination to construct long-chain amino compounds. The reaction system exhibits remarkable versatility in substrate scope using a non-noble ruthenium catalyst with formate and isopropanol as hydrogen sources, making it an appealing method for drug synthesis and molecular modification. [ABSTRACT FROM AUTHOR]

Dichloromethane, as a readily available and inexpensive C1 synthon is proposed as a powerful building block for cyclopropanation of alkenes under mild conditions. Herein, we report a highly efficient and versatile dual photoredox system, involving a nickel aminopyridine coordination complex and a photocatalyst, for the cyclopropanation of aromatic olefins using dichloromethane, under visible‐light irradiation. The cyclopropanation protocol has been successfully applied at gram scale. Mechanistic studies suggest a Ni(II) pyridyl radical complex as the key intermediate for the homolytic cleavage of the Csp3−Cl bond, generating a chloromethyl radical that is captured by the olefin coupling partner. Our findings also highlight the versatility of this methodology. By directing the radical/polar crossover process, we were able to selectively drive the reaction towards either the formation of cyclopropyl derivatives or the corresponding non‐cyclic alkyl chloride products. The methodology also successfully apply to geminal dichloroalkanes, including the formation of spiro[2,2] compounds. Moreover, our methodology extends to the synthesis of deuterium‐labelled cyclopropanes, demonstrating its utility in isotopic labelling and broadening its applicability in chemical synthesis and drug development. [ABSTRACT FROM AUTHOR]

Methods for producing drugs directly at the cancer site, particularly using bioorthogonal metal catalysts, are being explored to mitigate the side effects of therapy. Albumin‐based artificial metalloenzymes (ArMs) catalyze reactions in living mice while protecting the catalyst in the hydrophobic pocket. Here, we describe the in situ preparation and application of biocompatible tumor‐targeting ArMs using circulating albumin, which is abundant in the bloodstream. The ArM was formed using blood albumin through the intravenous injection of ruthenium conjugated with an albumin‐binding ligand; the tumor‐targeting unit was conjugated to the ArM using its catalytic activity, and the ArM was transported to the cancer site. The delivered ArM catalyzed a second tagging reaction of the proapoptotic peptide on the cancer surface, successfully suppressing cancer proliferation. This approach, which efficiently leveraged the persisting reactivity twice in vivo, holds promise for future in vivo metal‐catalyzed drug synthesis utilizing endogenous albumin. [ABSTRACT FROM AUTHOR]

The use of (para)-formaldehyde for the methylation/alkylation of C(sp2)–H and N–H bonds, utilizing a combination of silane and hexafluoroisopropanol (HFIP) as activators, is reported. Overcoming the complexity of C(sp2)–H methylation on aryl and indole substrates, the process utilizes a Friedel–Crafts alkylation, followed by silane as a hydride donor, under a mild acidic medium. The method has been employed for the synthesis of the antifungal drug butenafine and a derivative of the non-steroidal anti-inflammatory drug (NSAID) flurbiprofen. [ABSTRACT FROM AUTHOR]

Chiral tertiary alcohols are an important structural motif, however, the general and efficient methodologies for their synthesis are less reported. Herein, we report a Ni(ІІ)-catalyzed asymmetric alkenylation and arylation of aryl ketones with organoborons under air via a 1,5-metalate shift strategy to obtain chiral tertiary allylic alcohols and diaryl alcohols. The reaction demonstrates good functional group tolerance and delivers chiral tertiary alcohols with good to excellent results. Furthermore, this method can be applied to the late-stage modification of drugs and the efficient synthesis of natural products. Notably, the reaction proceeds through an outer-sphere mechanism. The Ni(II) complex functions both as a Lewis acid to activate the ketone and create a chiral environment, and as coordination bridge linking the ketone and the organoboron-derived "ate" complex, facilitating the 1,5-metalate shift without forming a C-Ni bond. This approach contrasts with traditional transition metal-catalyzed nucleophilic addition reactions that involve carbon-metal bond formation. Chiral tertiary alcohols are an important structural motif, but the general methodologies for the synthesis are less reported. Herein, the authors report a Ni(ІІ)-catalyzed asymmetric alkenylation and arylation of aryl ketones with organoborons under air via a 1,5-metalate shift to obtain chiral tertiary allylic alcohols and diaryl alcohols. [ABSTRACT FROM AUTHOR]

Site‐selective amination of N‐heterocycles is an interesting topic in organic synthesis and drug discovery. We herein present a method for the vicarious‐type nucleophilic amination of azine N‐oxides and cyclic iminoamides using iminyl anions, readily generated from organic azides under basic conditions. The plausible reaction mechanism involving nucleophilic aromatic substitution by iminyl anions is elucidated by a series of mechanistic investigations. [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]

In this study, a Ni‐based metal‐organic framework (MOF), Ni‐MOF, was synthesized from a mixture of Ni(OAc)2 ⋅ 4H2O, a dicarboxylate, 4,4'‐(1,3,4‐oxadiazole‐2,5‐diyl)dibenzoate (oxdz2−), and a bis(tridentate) ligand, (N,N',N",N"'‐tetrakis(2‐pyridylmethyl)‐1,4‐diaminoxylylene) (tpxn), under ambient conditions using greener solvents in 12 h. The framework was well‐characterized using several analytical techniques. The highly crystalline Ni‐MOF exhibited remarkable polarizing traits with significant uptake of CO2 and water vapor up to 10.53 cm3 g−1 and 290 cm3 g−1, respectively, at 298 K. The isosteric heat of adsorption between Ni‐MOF and CO2 at zero loading was calculated to be 32.43 kJ mol−1. Furthermore, utilizing its CO2‐philic and catalytic features, Ni‐MOF was employed as an excellent heterogeneous catalyst (2.5 mol%) along with very low concentration of TBAB (0.02 mmol) as a co‐catalyst for the synthesis of oxazolidinones via a standard three‐component reaction among an epoxide, a substituted aniline, and carbon dioxide under solvent‐free conditions. A wide range of oxazolidinones including three bioactive derivatives was synthesized using both diverse epoxides and aniline derivatives to demonstrate the substrate scope. The catalyst was proved to be recyclable, reusable, and stable for multiple cycles, without leaching of the metal from it. The mechanistic insights revealed that Ni‐MOF polarizes all three reactants to catalyze the oxazolidinone formation. [ABSTRACT FROM AUTHOR]

The excessive and prolonged use of antibiotics contributes to the emergence of drug‐resistant S. aureus strains and potential dysbacteriosis‐related diseases, necessitating the exploration of alternative therapeutic approaches. Herein, we present a light‐activated nanocatalyst for synthesizing in situ antimicrobials through photoredox‐catalytic click reaction, achieving precise, site‐directed elimination of S. aureus skin infections. Methylene blue (MB), a commercially available photosensitizer, was encapsulated within the CuII‐based metal–organic framework, MOF‐199, and further enveloped with Pluronic F‐127 to create the light‐responsive nanocatalyst MB@PMOF. Upon exposure to red light, MB participates in a photoredox‐catalytic cycle, driven by the 1,3,5‐benzenetricarboxylic carboxylate salts (BTC−) ligand presented in the structure of MOF‐199. This light‐activated MB then catalyzes the reduction of CuII to CuI through a single‐electron transfer (SET) process, efficiently initiating the click reaction to form active antimicrobial agents under physiological conditions. Both in vitro and in vivo results demonstrated the effectiveness of MB@PMOF‐catalyzed drug synthesis in inhibiting S. aureus, including their methicillin‐resistant strains, thereby accelerating skin healing in severe bacterial infections. This study introduces a novel design paradigm for controlled, on‐site drug synthesis, offering a promising alternative to realize precise treatment of bacterial infections without undesirable side effects. [ABSTRACT FROM AUTHOR]

Sulfonamides have been played a critical role in the history of medicinal chemistry development for decades. In particular, sulfonamides display a broad spectrum in pharmaceutical drugs synthesis. This review presents a short discussion of the microwave‐assisted synthetic approaches, enhancement of sulfonamides moieties and their pharmacological applications are being discussed. During the past few decades, microwave‐assisted technology in organic synthesis has been highlighted to introducing ‐SO2NH functional group in the multi synthetic routes for the development of bioactive molecule and also assisted in the estimation of their credible mechanistic routes for the reactions. [ABSTRACT FROM AUTHOR]

A diastereoselective synthesis for the preparation of (R)‐methyl pipecolate and dextro‐erythrophacetoperane, analogs of methylphenidate, drugs used to treat attention deficit hyperactivity disorder, is reported. The key steps involve a high diastereoselective ring‐closing reaction via enolate formation and a diastereoselective ketone reduction reaction. The total synthesis of these valuable drugs could be obtained in only 5 and 8 steps, respectively, starting from (S)‐(−)‐methyl benzylamine. [ABSTRACT FROM AUTHOR]

Deuteration has emerged as a significant method for investigating kinetic isotope effects in chemical reactions. In recent years, research on deuteration has revealed that this reaction often alters the pharmacokinetic or toxicological properties of drug molecules, thereby enhancing their therapeutic effect. Therefore, deuteration is considered as a potential avenue for drug research direction. Since the approval of the first deuterated drug, "deutetrabenazine," by the American Food and Drug Administration (FDA) in 2017, deuteration has been applied in the development of a variety of novel drugs. Research on deuteration technology has matured with the publication of numerous deuteration strategies. This article reviews recently reported strategies for late‐stage selective deuteration, discusses the challenges associated with current deuteration strategies, and presents future prospects for the synthesis of deuterated drugs. [ABSTRACT FROM AUTHOR]

Thiazole derivatives have long been a hot topic in pharmaceutical research and remain among the greatest active fields in heterocyclic chemistry. Thiazole derivatives, as one of the potentially favored structure, have been extensively desirable by industrial and medicinal researchers and have gained significant success in the previous decades due to their various biological activities, such as anticancer, antibacterial, antifungal, anti-HIV, antiulcer, and anti-inflammatory activity. In addition, many thiazole drugs are well-known pharmaceuticals on the market. This review summarizes the freshly synthesized routes and prospective biological activities of thiazole derivatives. In addition, it highlights thiazoles as treatment drugs in clinical trials or approved by the FDA and spotlights on some of their industrial applications. On the other hand, one of the goals of this review is to open up prospects for the future design, development, and usage of thiazole derivatives as potent drugs. [ABSTRACT FROM AUTHOR]

(R)-3-Isobutylglutarate monoamide (R-IBM) is a key intermediate in the synthesis of the analgesic drug pregabalin. Recently, the imidase BpIH derived from Burkholderia phytofirmans was identified as a promising catalyst for the industrial production of R-IBM. Notably, this catalyst has the distinct advantage of achieving a 100% theoretical yield from 3-isobutyl glutarimide (IBI). In this study, homology modeling and structure alignment techniques were used to determine the substrate binding pocket of BpIH. Semi-rational design was used to analyze the amino acid residue conservation in the binding pocket region of BpIH. Interestingly, mutations of several low-conserved amino acid located 6–9 Å from the substrate significantly enhanced the catalytic activity of BpIH. Among them, the triple mutant Y37FH133NS226I (YHS-I) showed approximately a fivefold increase in enzyme activity and a significantly improved catalytic efficiency (kcat/Km). Under the same reaction time and conditions, YHS-I successfully converted IBI into R-IBM with a conversion rate of 88.87%, with an enantiomeric excess (ee) of the product exceeding 99.9%. In comparison, wild-type BpIH had a conversion rate of only 38.15%. Molecular dynamics and docking results indicated that YHS-I had higher rigidity around the mutation sites. The synergistic substitutions of Y37F, H133N, and S226I altered the interaction network within the mutation site, enhancing the protein's affinity for the substrate and improving catalytic efficiency. Key points: • 100% theoretical yield of R-IBM by BpIH compared with 50% by resolution • Semi-rational design of BpIH based on conservativity with homologous enzymes • Mutant with enzyme activity of sixfold and product ee value of 99.9% [ABSTRACT FROM AUTHOR]

The photochemistry of EDA complexes is initiated from a groundstate associate with a biomolecule capable of intermolecular electron transfer by channelling chemical synthesis via a specific radical-based mechanistic pathway. Herein, we activate the innovative cascade mode of EDA complex photoexcitation for nitroreduction in aqueous media using charge transfer interactions between a sole donor and multiple acceptors (ArNO2, ArNO, and ArNHOH·glycine adduct). A triplet-state quenching experiment, UV-vis analysis, NMR titration, and preliminary kinetic investigation verified the rationality and feasibility of the mechanism. With successful applications of this cascaded system in arylamine compounds and commercially available drug synthesis (61 examples), these achievements highlight the attractiveness, usefulness, and effectiveness of this protocol. [ABSTRACT FROM AUTHOR]

Comprehensive Summary: Unsymmetrical diarylamines are crucial components in many pharmaceuticals and functional materials. In this study, we introduce an efficient Chan‐Lam cross‐coupling method that utilizes phenylboronic acids and aryl azides as coupling agents in a redox‐neutral environment, enabled by a synergistic nickel/photoredox catalytic system. This approach leverages a proton‐coupled electron transfer mechanism to bypass the typical nitrene pathway associated with aryl azides, which is prone to intramolecular rearrangement, C—H amination, and reductive hydrogenation. Notably, our method exhibits broad compatibility with a variety of functional groups, including those derived from pharmaceuticals, demonstrating its versatile potential in organic synthesis and drug modification. [ABSTRACT FROM AUTHOR]

Comprehensive Summary: In this paper, the difunctionalizative perfluoroalkyloximation of alkenes has been developed for the first time. This photochemical method allows for the synthesis of various perfluoroalkyl ethanone oximes with excellent regioselectivity and good functional group tolerance. Our method employs the most common perfluoroalkyl source, perfluoroalkyl iodides, as Rf reagents. Besides long‐chain perfluoroalkyl groups, this approach could be extended to incorporating additional groups, including trifluoromethyl, difluoromethyl, sulfonyl, and malonate, selectively into olefins, resulting in a range of β‐substituted ethanone oximes. Notably, the potential of this method in the Fukuyama indole synthesis, generating novel 2‐perfluoroalkylated 3‐(α‐oximidobenzyl)indoles via a radical cascade mechanism with 2‐vinylphenylacryloyl isocyanate as the radical acceptor, presents a compelling avenue for drug synthesis. The protocol is efficient, scalable, and useful for late‐stage modification of bioactive molecules. [ABSTRACT FROM AUTHOR]

Atropisomers have attracted a great deal of attention lately due to their numerous applications in organic synthesis and to their employment in drug discovery. However, the synthetic arsenal at our disposal with which to access them remains limited. The research described herein is two‐pronged; we both demonstrate the use of MCR chemistry as a synthetic strategy for the de novo synthesis of a class of atropisomers having high barriers to rotation with the simultaneous insertion of multiple chiral elements and we study these unprecedented molecular systems by employing a combination of crystallography, NMR and DFT calculations. By fully exploiting the synthetic capabilities of our chemistry, we have been able to monitor a range of different types of interaction, i. e. π‐π, CH–π, heteroatom‐π and CD–π, in order to conduct structure‐property studies. The results could be applied both to atroposelective synthesis and in drug discovery. [ABSTRACT FROM AUTHOR]

Nucleoside phosphorylases (NPs) are pivotal enzymes in the salvage pathway, catalyzing the reversible phosphorolysis of nucleosides to produce nucleobases and α-D-ribose 1-phosphate. Due to their efficiency in catalyzing nucleoside synthesis from purine or pyrimidine bases, these enzymes hold significant industrial importance in the production of nucleoside-based drugs. Given that the thermodynamic equilibrium for purine NPs (PNPs) is favorable for nucleoside synthesis—unlike pyrimidine NPs (PyNPs, UP, and TP)—multi-enzymatic systems combining PNPs with PyNPs, UPs, or TPs are commonly employed in the synthesis of nucleoside analogs. In this study, we report the first development of two engineered bifunctional fusion enzymes, created through the genetic fusion of purine nucleoside phosphorylase I (PNP I) and thymidine phosphorylase (TP) from Thermus thermophilus. These fusion constructs, PNP I/TP-His and TP/PNP I-His, provide an innovative one-pot, single-step alternative to traditional multi-enzymatic synthesis approaches. Interestingly, both fusion enzymes retain phosphorolytic activity for both purine and pyrimidine nucleosides, demonstrating significant activity at elevated temperatures (60–90 °C) and within a pH range of 6–8. Additionally, both enzymes exhibit high thermal stability, maintaining approximately 80–100% of their activity when incubated at 60–80 °C over extended periods. Furthermore, the transglycosylation capabilities of the fusion enzymes were explored, demonstrating successful catalysis between purine (2′-deoxy)ribonucleosides and pyrimidine bases, and vice versa. To optimize reaction conditions, the effects of pH and temperature on transglycosylation activity were systematically examined. Finally, as a proof of concept, these fusion enzymes were successfully employed in the synthesis of various purine and pyrimidine ribonucleoside and 2′-deoxyribonucleoside analogs, underscoring their potential as versatile biocatalysts in nucleoside-based drug synthesis. [ABSTRACT FROM AUTHOR]

Some antibiotics that are frequently employed are β-lactams. In light of the hydrolytic process of β-lactamase, found in Gram-negative bacteria, inhibitors of β-lactamase (BLIs) have been produced. Examples of first-generation β-lactamase inhibitors include sulbactam, clavulanic acid, and tazobactam. Many kinds of bacteria immune to inhibitors have appeared, and none cover all the β-lactamase classes. Various methods have been utilized to develop second-generation β-lactamase inhibitors possessing new structures and facilitate the formation of diazabicyclooctane (DBO), cyclic boronate, metallo-, and dual-nature β-lactamase inhibitors. This review describes numerous promising second-generation β-lactamase inhibitors, including vaborbactam, avibactam, and cyclic boronate serine-β-lactamase inhibitors. Furthermore, it covers developments and methods for synthesizing MβL (metallo-β-lactamase inhibitors), which are clinically effective, as well as the various dual-nature-based inhibitors of β-lactamases that have been developed. Several combinations are still only used in preclinical or clinical research, although only a few are currently used in clinics. This review comprises materials on the research progress of BLIs over the last five years. It highlights the ongoing need to produce new and unique BLIs to counter the appearance of multidrug-resistant bacteria. At present, second-generation BLIs represent an efficient and successful strategy. [ABSTRACT FROM AUTHOR]

Potential genotoxic impurities in medications are an increasing concern in the pharmaceutical industry and regulatory bodies because of the risk of human carcinogenesis. To prevent the emergence of these impurities, it is crucial to carefully examine not only the final product but also the intermediates and key starting material (KSM) used in drug synthesis. During the related substances analysis of KSM of Famotidine, an unknown impurity in the range of 0.5–1.0% was found prompting the need for isolation and characterization due to the possibility of its to infiltrate into the final product. In this study, the impurity was isolated and characterized as 5-(2-chloroethyl)-3,3-dimethyl-3,4-dihydro-2H-1,2,4,6-thiatriazine 1,1-dioxide using multiple instrumental analysis, uncovering a structural alert that raises concern. Considering the potential impact of impurity on human health, an in silico genotoxicity assessment was established using Derek and Sarah tool in accordance with ICH M7 guideline. Furthermore, molecular docking and molecular dynamics simulation were performed to evaluate the specific interaction of the impurity with DNA. The findings reveal consistent interaction of the impurity with the dG-rich region of the DNA duplex and binding at the minor groove. Both in silico prediction and molecular dynamic study confirmed the genotoxic character of the impurity. The newly discovered impurity in famotidine has not been reported previously, and there is currently no analytical method available for its identification and control. A highly sensitive HPLC-UV method was developed and validated in accordance with ICH requirements, enabling quantification of the impurity at trace level in famotidine ensuring its safe release. [ABSTRACT FROM AUTHOR]

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A regioselective novel one-pot synthesis of heterocyclic purine derivative antiviral agent Ganciclovir in which initially guanine is treated with acetic anhydride in the presence of iodine (5%) to get diacetyl guanine intermediate, which undergoes in situ N-alkylation with AMDP in presence of catalytic acidic Amberlite IR-120 to get N-alkylated intermediate and finally deacetylation to get pure regioselective Ganciclovir, which is commercially viable and eco-friendly. We developed one-pot synthesis of antiviral drug Ganciclovir. Initially, Guanine is treated with acetic anhydride and iodine to yield diacetyl guanine 3. This intermediate then reacted with AMDP in the presence of acidic Amberlite IR-120 to obtain compound 5. Finally, deacetylation yields Ganciclovir 1, a commercially viable and eco-friendly process. [ABSTRACT FROM AUTHOR]

AbstractProblem StatementMethodResultsDiscussionPublic Statement of RelevanceAmong individuals aged 12 years or older, 14.3% (40.0 million) reporting the use of an illicit drug in the previous year. Given the prevalence of drug abuse, it is increasingly important to determine effective screening practices, treatment procedures, and best practices among various subpopulations to identify drug use-related consequences. The DAST is one of the most commonly used and accurate drug screening tests.This psychometric synthesis of four versions of the Drug Abuse Screening Test (DAST-10, DAST-20, DAST-28, DAST-A) provided aggregated evidence from 346 articles over 40 years of published literature for score reliability, structure, diagnostic, and convergent validity, and descriptive statistics, all with the goal of informing counseling and medical practice and research.Results indicated adequate internal consistency (α = 0.81–0.84 across all four versions) and mostly medium to large effect size convergent correlations with comparison measures. Aggregated diagnostic validity data indicate optimal cutoff scores of 7 for DAST-10, 8 for DAST-20, 10 for DAST-28, and 6 for DAST-A.The DAST-10 appears the best choice for practical and psychometric reasons. Additional studies of the various DAST versions are needed to expand use across participant demographics.Drug use continues to be a societal problem and mental health practitioners need effective screening practices, treatment procedures, and best practices among various subpopulations to identify drug use-related consequences. This study synthesized 40 years of research on the four versions of the Drug Abuse Screening Test (DAST-10, DAST-20, DAST-28, DAST-A) and found acceptable levels of score reliability and validity for screening purposes. [ABSTRACT FROM AUTHOR]

Sulfinamidines are promising aza‐SIV chiral building blocks in asymmetric synthesis and drug discovery. However, no report has documented their enantioselective synthesis. Here we present an enantioselective synthesis of sulfinamidines via electrophilic amination of sulfenamides using an enantiopure N−H oxaziridine. The resulting enantiomerically enriched primary sulfinamidines are configurationally stable at 90 °C in solution and show remarkable stability against organic acids and bases under non‐aqueous conditions. We also demonstrate a one‐pot, three‐component, enantioselective synthesis of sulfinamides using N−H oxaziridine reagents. [ABSTRACT FROM AUTHOR]

In this communication, we designed a highly selective camphor sulfonyl functionalized crown-ether-tethered calix[4]arene-derived organocatalyst for asymmetric Strecker reaction to provide the desired cyano adducts in high yields (∼99.9% yield) and enantioselectivities (up to 99.3% ee). Furthermore, 2 step facile syntheses of the antiplatelet drug (S)-clopidogrel exemplify the potential of this method for the preparation of commercial compounds. [ABSTRACT FROM AUTHOR]

The reagent system based on the combined use of Et3SiH/I2 acts as an efficient N-glycosidation promoter for the synthesis of natural and sugar-modified nucleosides. An analysis of reaction stereoselectivity in the absence of C2-positioned stereodirecting groups revealed high selectivity with six-membered substrates, depending on the nucleophilic character of the nucleobase or based on anomerization reactions. The synthetic utility of the Et3SiH/I2-mediated N-glycosidation reaction was highlighted by its use in the synthesis of the investigational drug apricitabine. [ABSTRACT FROM AUTHOR]

During gliotoxin biosynthesis in fungi, the cytochrome P450 GliF enzyme catalyzes an unusual C–N ring-closure step while also an aromatic ring is hydroxylated in the same reaction cycle, which may have relevance to drug synthesis reactions in biotechnology. However, as the details of the reaction mechanism are still controversial, no applications have been developed yet. To resolve the mechanism of gliotoxin biosynthesis and gain insight into the steps leading to ring-closure, we ran a combination of molecular dynamics and density functional theory calculations on the structure and reactivity of P450 GliF and tested a range of possible reaction mechanisms, pathways and models. The calculations show that, rather than hydrogen atom transfer from the substrate to Compound I, an initial proton transfer transition state is followed by a fast electron transfer en route to the radical intermediate, and hence a non-synchronous hydrogen atom abstraction takes place. The radical intermediate then reacts by OH rebound to the aromatic ring to form a biradical in the substrate that, through ring-closure between the radical centers, gives gliotoxin products. Interestingly, the structure and energetics of the reaction mechanisms appear little affected by the addition of polar groups to the model and hence we predict that the reaction can be catalyzed by other P450 isozymes that also bind the same substrate. Alternative pathways, such as a pathway starting with an electrophilic attack on the arene to form an epoxide, are high in energy and are ruled out. [ABSTRACT FROM AUTHOR]

Phenolic compounds have long captivated the interest of organic synthesis, particularly in their quest for selective hydroxylation of arenes using H2O as a hydroxyl source. However, the inherent high reactivity and low redox potential of phenols often lead to undesirable overoxidation byproducts. To address this challenge, herein, we develop an electrophotochemical approach, finetuning substrate oxidative potential and enabling para-selective hydroxylation of anilides. This method showcases versatility, accommodating a wide array of substrates, while revealing high regional selectivity and compatibility with diverse functional groups. Moreover, the protocol allows facile late-stage functionalization of biologically active molecules. Mechanistic investigations demonstrate the activation of anilides by the excited state photocatalyst, effectively decreasing their oxidative potential and enhancing regional selectivity during hydroxylation. By using this protocol, important drug molecules such as Paracetamol, Fenretinide, Practolol, and AM404 could be synthesized, demonstrating the applicability of this approach in drug synthesis and late-stage functionalization. Phenolic compounds have long captivated the interest of organic synthesis, particularly in their quest for selective hydroxylation of arenes using H2O as a hydroxyl source but the inherent high reactivity and low redox potential of phenols often lead to undesirable overoxidation byproducts. Here the authors develop an electrophotochemical approach, finetuning substrate oxidative potential and enabling para-selective hydroxylation of anilides. [ABSTRACT FROM AUTHOR]

A green, efficient and highly regioselective synthesis of flavonoids and their derivatives from β-phenoxyl ynones using wet 1,3-propanediol as reaction medium was developed, without any metal catalysts, bases, acids or additives. The reaction shows a high level of functional tolerance and a broad substrate scope, with simple operation and high atomic economy. Furthermore, a mechanism study has shown that 1,3-propanediol acts both as a participant and solvent to achieve regioselective cyclization and carbonyl site oxygen migration. Significantly, the total synthesis of drug molecules efloxate 6 and flavodilol 7 and bioactive molecules, such as 8 and MN-64, further demonstrates the efficacy and synthetic potential of this method. Moreover, most established flavonoid derivatives are found to have strong anti-inflammatory activities, during which 2d exhibits a better result with lower IC50 value of 5.67 μg mL−1. [ABSTRACT FROM AUTHOR]

The reduction of aromatic compounds constitutes a fundamental and ongoing area of investigation. The selective reduction of polycyclic aromatic compounds to give either fully or partially reduced products remains a challenge, especially in applications to complex molecules at scale. Herein, we present a selective electrochemical hydrogenation of polycyclic arenes conducted under mild conditions. A noteworthy achievement of this approach is the ability to finely control both the complete and partial reduction of specific aromatic rings within polycyclic arenes by judiciously varying the reaction solvents. Mechanistic investigations elucidate the pivotal role played by in situ proton generation and interface regulation in governing reaction selectivity. The reductive electrochemical conditions show a very high level of functional‐group tolerance. Furthermore, this methodology represents an easily scalable reduction (demonstrated by the reduction of 1 kg scale starting material) using electrochemical flow chemistry to give key intermediates for the synthesis of specific drugs. [ABSTRACT FROM AUTHOR]

Comprehensive Summary: Herein, we present a method for the homogeneous hydrogenation of nitroarenes to produce anilines using low catalyst loading (1 mo%) of copper N‐heterocyclic carbene complexes as the catalyst and ammonia borane as the source of hydrogen. A wide range of nitroarenes, featuring diverse functional groups, were selectively transformed into their corresponding primary aromatic amines with high yields. This process can be readily scaled up and exhibits compatibility with various sensitive functional groups, including halogen, trifluoromethyl, aminomethyl, alkenyl, cyano, ester, amide, and hydroxyl. Notably, this catalytic methodology finds application in the synthesis of essential drug compounds. Mechanistic investigations suggest that the in‐situ‐generated Cu‐H species may serve as active intermediates, with reduction pathways involving species such as azobenzene, 1,2‐diphenylhydrazine, nitrosobenzene, and N‐phenylhydroxylamine. [ABSTRACT FROM AUTHOR]

Infections with Flaviviridae viruses, such as hepatitis C (HCV), dengue (DENV), and yellow fever (YFV) viruses, are major public health problems worldwide. In the case of HCV, treatment is associated with drug resistance and high costs, while there is no clinically approved therapy for DENV and YFV. Consequently, there is still a need for new chemotherapies with alternative modes of action. We have previously identified novel 2-hydroxypyrazino[1,2-a]indole-1,3(2H,4H)-diones as metal-chelating inhibitors targeting HCV RNA replication. Here, by utilizing a structure-based approach, we rationally designed a second series of compounds by introducing various substituents at the indole core structure and at the imidic nitrogen, to improve specificity against the RNA-dependent RNA polymerase (RdRp). The resulting derivatives were evaluated for their potency against HCV genotype 1b, DENV2, and YFV-17D using stable replicon cell lines. The most favorable substitution was nitro at position 6 of the indole ring (compound 36), conferring EC50 1.6 μM against HCV 1b and 2.57 μΜ against HCV 1a, with a high selectivity index. Compound 52, carrying the acetohydroxamic acid functionality (-CH2CONHOH) on the imidic nitrogen, and compound 78, the methyl-substituted molecule at the position 4 indolediketopiperazine counterpart, were the most effective against DENV and YFV, respectively. Interestingly, compound 36 had a high genetic barrier to resistance and only one resistance mutation was detected, T181I in NS5B, suggesting that the compound target HCV RdRp is in accordance with our predicted model. [ABSTRACT FROM AUTHOR]

This study explores the medicinal potential of Pergularia daemia, a perennial vine abundant along Indian roadsides, focusing on its leaves have diverse therapeutic properties in traditional medicine. This research investigates its unexplored potential in application of drug delivery and the synthesis of zinc oxide nano-particles from its leaves. PD mediated Zinc Oxide nanoparticles were synthesized by precipitate method. The qualitative phyto chemical analysis of PD leaves extract was carried out and the extract showed the presence of carbohydrates, phenols, flavanoids, alkaloids and terpenoids. The synthesized zinc oxide nanoparticles were characterized by UV–Visible spectroscopy, Fourier transform Infrared spectroscopy, X-ray diffraction Analysis and scanning electron microscope. The results from characterization suggest that the synthesized compound was ZnO in nano scale which was in oval shape and with high purity. The synthesized zinc oxide nano particle could be a huge application in medical field, pharmaceutical and biotechnology in near future. [ABSTRACT FROM AUTHOR]

Human liver subcellular fractions, including liver microsomes (HLM), liver cytosol fractions, and S9 fractions, are extensively utilized in in vitro assays to predict liver metabolism. The S9 fractions are supernatants of human liver homogenates that contain both microsomes and cytosol, which include most cytochrome P450 (CYP) enzymes and soluble phase II enzymes such as glucuronosyltransferases and sulfotransferases. This study reports on the direct electrochemistry and biocatalytic features of redox-active enzymes in S9 fractions for the first time. We investigated the electrochemical properties of S9 films by immobilizing them onto a high-purity graphite (HPG) electrode and performing cyclic voltammetry under anaerobic (Ar-saturated) and aerobic (O2-saturated) conditions. The heterogeneous electron transfer rate between the S9 film and the HPG electrode was found to be 14 ± 3 s−1, with a formal potential of −0.451 V vs. Ag/AgCl reference electrode, which confirmed the electrochemical activation of the FAD/FMN cofactor containing CYP450-reductase (CPR) as the electron receiver from the electrode. The S9 films have also demonstrated catalytic oxygen reduction under aerobic conditions, identical to HLM films attached to similar electrodes. Additionally, we investigated CYP activity in the S9 biofilm for phase I metabolism using diclofenac hydroxylation as a probe reaction and identified metabolic products using liquid chromatography–mass spectrometry (LC-MS). Investigating the feasibility of utilizing liver S9 fractions in such electrochemical assays offers significant advantages for pharmacological and toxicological evaluations of new drugs in development while providing valuable insights for the development of efficient biosensor and bioreactor platforms. [ABSTRACT FROM AUTHOR]

The beginning of photochemical reactions revolutionized synthetic chemistry through sustainable practices. This review explores cutting‐edge developments in leveraging light‐induced processes for generating cascaded C−C and C‐hetero bonds without catalysts. Significantly, catalyst‐free photoinduced methodologies have garnered considerable attention, especially in the creation of varied heterocyclic frameworks for drug design and the synthesis of natural products. The article delves into underlying mechanisms, addresses limitations, and evaluates various methodologies, emphasizing the potential of photocatalyst and transition metal‐free photochemical reactions to enhance sustainability. Divided into two sections, it covers recent strides in C−C and C‐heteroatom and multiple C‐heteroatom bond formation reactions. [ABSTRACT FROM AUTHOR]

Electrically controlled droplet manipulation is attractive for lots of applications ranging from material synthesis and drug delivery. However, the present techniques using bulky and expensive power supplies to generate high‐voltage electrical signals are easy to cause electrode electrolysis, bubble formation in buffer solution, and are incapable for point‐of‐care testing. Herein, a novel and portable electrical method for self‐powered emulsion droplet core coalescence and release based on triboelectric nanogenerator (TENG) is presented. The electrical signal with a 2.25 kV open‐voltage and a 35 µA short‐circuit current can be conveniently generated via frictional electrification effect, and the harmful electrochemical reaction in solutions can be avoided. The high transient pulse voltage and stable sinusoidal signal between two electrodes in microfluidic device can generate a strong electric field, which causes apparent Maxwell electrical stresses at droplet interfaces and subsequently promotes the core coalescence and release of double‐emulsions. By adjusting the voltage magnitude, the core coalescence and release behaviors of double‐emulsion droplets can be controllably achieved, followed by the synthesis copper‐based metal–organic framework (Cu‐MOF) nanoparticles. Thus, this portable, effective and self‐powered droplet manipulation technique can be attractive for those droplet‐based applications. [ABSTRACT FROM AUTHOR]

Alkylamine structures represent one of the most functional and widely used in organic synthesis and drug design. However, the general methods for the functionalization of the shielded and deshielded alkyl radicals remain elusive. Here, we report a general deoxygenative amination protocol using alcohol-derived carbazates and nitrobenzene under electrochemical conditions. A range of primary, secondary, and tertiary alkylamines are obtained. This practical procedure can be scaled up through electrochemical continuous flow technique. Secondary arylalkylamines represent important building blocks for organic synthesis, and as such their straightforward synthesis from readily available chemicals remains a priority in organic chemistry. Here, the authors report a synthesis of arylalkylamines from nitroarenes and carbazates via paired electrolysis. [ABSTRACT FROM AUTHOR]

Novel biocompatible systems suitable for the controlled release of active ingredients are under the spotlight within the last few years. The present investigation focuses on the preparation of nanoparticles (NPs) based on the amphiphilic copolymer pullulan‐graft‐poly(Z‐L‐lysine) bearing different amounts of lysine (10, 20, and 30 wt%), and on the evaluation of their ensuing viability to encapsulate the hydrophobic nonsteroidal anti‐inflammatory drug indomethacin (INDO). The copolymers are synthesized by ring‐opening polymerization, characterized by NMR and FTIR, and their critical aggregation concentration is determined by fluorescence. The NPs are prepared with and without INDO using different copolymer/solvent ratios and INDO/copolymer ratios. The hydrodynamic diameter and polydispersity of the NP suspensions are monitored by dynamic light scattering for 30 days. Their sizes vary between 208 and 338 nm, and some reach the micrometric range (19–73 μm). INDO‐free NPs are identified as spherical‐shaped by atomic force microscopy. Two formulations are tested in terms of encapsulation efficiency (EE = 43%–89%), and the drug crystallinity (DC = 7%–27%) which is determined by differential scanning calorimetry, indicating a reduction with respect to pristine INDO. The results suggest that the copolymers prepared herewith have potential to be applied as carriers for new drug delivery systems of class II drugs. [ABSTRACT FROM AUTHOR]

Bilastine (BLA), 2-(4-(2-(4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazole-2-yl)-piperidin-1-yl)-ethyl)-phenyl)-2-methylpropanoic acid, is an active antihistamine drug. With the idea of repurposing drugs from the existing pool of 'active' pharmaceutical ingredients, the therapeutic potency of bilastine as an anticancer agent was investigated via the tailored synthesis of a metal-based anticancer drug formulation of the type [BLA(phen)2M(II)]+·X−, where M = Co, Cu, and Zn and X− = NO3 and ClO4. The synthesized metal-based chemotherapeutics derived from the bilastine drug that acts as a ligand were thoroughly characterized using spectroscopic techniques, namely, UV-vis, FT-IR, and EPR (in the case of 1 and 2); 1H-NMR and 13C-NMR (in the case of 3); ESI-MS and single-crystal X-ray diffraction studies. Comprehensive biological studies (DNA binding, cleavage, and cytotoxic activity) using various biophysical and gel electrophoretic methods were carried out to validate their potential as anticancer agents. The cytotoxic activity of 'therapeutically promising' copper(II)-based drug candidate 2 was evaluated against MCF-7, MBA-MD-231, HeLa, HepG2, and Mia-PaCa-2 cancer cells via an SRB assay, and the results demonstrated 2 as a potent anticancer agent at low nanomolar concentrations against all tested cancer cells, preferably with a much superior anticancer efficacy against human pancreatic cancer cells. [ABSTRACT FROM AUTHOR]

Multicomponent tandem reactions have become indispensable synthetic methods due to their economic advantages and efficient usage in natural products and drug synthesis. The emergence of metalated covalent organic frameworks (MCOFs) has opened up new opportunities for the advancement of multicomponent tandem reactions. In contrast to commonly used homogeneous transition metal catalysts, MCOFs possess regular porosity, high crystallinity, and rich metal chelation sites that facilitate the uniform distribution and anchoring of metals within their cavities. Thus, they show extremely high activity and have recently been widely employed as catalysts for multicomponent tandem reactions. It is timely to conduct a review of MCOFs in multicomponent tandem reactions, in order to offer guidance and assistance for the synthesis of MCOF catalysts and their application in multicomponent tandem reactions. This review provides a comprehensive overview of the design and synthesis of MCOFs, their application and progress in multicomponent tandem reactions, and the primary challenges encountered during their current development with the aim of contributing to the promotion of the field. [ABSTRACT FROM AUTHOR]

Dearomatization has emerged as a powerful tool for rapid construction of 3D molecular architectures from simple, abundant, and planar (hetero)arenes. The field has evolved beyond simple dearomatization driven by new synthetic technology development. With the renaissance of photocatalysis and expansion of the activation mode, the last few years have witnessed impressive developments in innovative photochemical dearomatization methodologies, enabling skeletal modifications of dearomatized structures. They offer truly efficient and useful tools for facile construction of highly complex structures, which are viable for natural product synthesis and drug discovery. In this review, we aim to provide a mechanistically insightful overview on these innovations based on the degree of skeletal alteration, categorized into dearomative functionalization and skeletal editing, and to highlight their synthetic utilities. [ABSTRACT FROM AUTHOR]

Tempted by the unique medicinal and biological potential of indole‐containing heterocycles, chemists, especially those specializing in heterocycle synthesis and drug discovery, are actively pursuing their efficient construction. This review spotlights the latest advancements in microwave‐assisted (M. W.) synthesis of diverse indole‐based heterocyclic compounds. We systematically categorize the reported methods based on the specific indole substitution patterns. This review concise the microwave assisted synthesis of indole based‐pyridine derivatives, indole based‐pyrimidine, indole based‐oxindole, spiro‐oxindole, Fischer indole Heck‐isomerization derivatives, functionalized indole, substituted indoles, indolyl quinoline, indole triazole and indolylnicotinonitriles derivatives. Ultimately, this review aims to provide organic and medicinal chemists with a concise yet informative guide to recent methodologies employing indole derivatives in the microwave‐powered synthesis of heterocycles. [ABSTRACT FROM AUTHOR]

A one‐pot Pd‐catalyzed tandem process to prepare (2‐arylallyl) aryl sulfones has been developed. This strategy is based on the modular assembly of a boronic acid, a sodium sulfinate and 2‐bromoallyl acetate. The reaction is completely regioselective towards the terminal alkene, yielding (2‐arylallyl) aryl (or alkyl) sulfones with yields ranging from 56 to 93%. Control experiments together with DFT calculations allowed to propose a plausible reaction mechanism of the tandem reaction. The usefulness of this methodology has been demonstrated with the formal synthesis of the marketed drug Apremilast and of several natural products by asymmetric hydrogenation. Using the commercially available UbaPHOX iridium complex, chiral β‐methyl sulfones with up to 98% ee were obtained [ABSTRACT FROM AUTHOR]

Atenolol, one of the top five best-selling drugs in the world today used to treat angina and hypertension, and to reduce the risk of death after a heart attack, faces challenges in current synthetic methods to address inefficiencies and environmental concerns. The traditional synthesis of this drug involves a process that generates a large amount of waste and other by-products that need disposal. This study presents a one-pot DES-based sustainable protocol for synthesizing atenolol. The use of the DES allowed the entire process to be conducted with no need for additional bases or catalysts, in short reaction times, under mild conditions, and avoiding chromatographic purification. The overall yield of atenolol was 95%. The scalability of the process to gram-scale production was successfully demonstrated, emphasizing its potential in industrial applications. Finally, the 'greenness' evaluation, performed using the First Pass CHEM21 Metrics Toolkit, highlighted the superiority in terms of the atom economy, the reaction mass efficiency, and the overall process mass intensity of the DES-based synthesis compared with the already existing methods. [ABSTRACT FROM AUTHOR]

Heteroatoms are very important in polyoxometalates (POMs) because they can lead to appealing architectures and unexpected properties in the final POMs. In this work, we elaborately designed and isolated three Silverton-type POMs ([UIVMo12O42] 8−) with UIV as the heteroatom and linked by FeII (FeUMo), CoII (CoUMo) and NiII (NiUMo). These Silverton-type U-containing polyoxomolybdates were demonstrated to be the first molecular catalysts for the synthesis of quinazolinone drug precursor skeletons. Under the optimized reaction conditions, 27 quinazolinones could be obtained in high yield with water as the sole by-product under mild conditions. Furthermore, NiUMo can be recycled seven times and still keep high stability and catalytic activity. [ABSTRACT FROM AUTHOR]

[Display omitted] Chemo-immunotherapy, in which chemotherapeutic drugs activate immune system to suppress tumor growth and metastases, has great potential for clinical application. However, insufficient immunogenic cell death and serious side effects caused by tumor multidrug resistance and non-specific drug distribution, as well as inadequate and dysfunctional immune cells, greatly impair the effectiveness of chemo-immunotherapy. Herein, taking advantage of the functional diversity and structural programmability of nucleic acids, a DNA-based bioorthogonal nanoagonist is constructed to initiate and augment immune responses for robust chemo-immunotherapy. Benefiting from polyvalent targeting and template effects of DNA, the tailor-made nanoagonist shows prior bioorthogonal catalytic performance. Chemotherapeutic drug is bioorthogonally synthesized in situ under the catalysis of the nanoagonist, maximizing immunogenic cell death and minimizing systemic toxicity. The large amount of antigen and damage-associated molecular patterns released from dying tumor cells effectively initiates antitumor immunity. Meanwhile, the integration of high density of immunologic adjuvant can more effectively stimulate immune cells. The combination of bioorthogonal catalytic drug synthesis and immunostimulatory effect of DNA adjuvant not only destroys local primary tumors, but also eliminates distal metastasis. Moreover, the nanoagonist triggered the immune memory effect. The work extends the application of bioorthogonal chemistry to immunotherapy and provides a safe and powerful strategy for cancer chemo-immunotherapy. [ABSTRACT FROM AUTHOR]

In this work, new substituted drugs polymerized as new homogenous polymers with study their medicinal properties to extend the controlled drug. The first step includes the preparation of compound N-(4-hydroxyphenyl) maleimide (D1) via a reaction of maleic anhydride with 4-aminophenol. Then compound (D1) was converted to maleimide phenol acetic acid ether (D2) which converted to its corresponding acyl chloride derivative which reacted with amino drugs (Ceftriaxone, Ciprofloxacin) afforded monomers (D3 and D4). Homogeneous polymers (D5 and D6) were prepared via free radical polymerization reaction of the monomers (D3, and D4) under nitrogen using Benzoyl peroxide (Bpo) as initiator. All these prepared monomers and polymers were characterized by FT-IR and 1H-NMR, 13C-NMR techniques and C.H.N.S. Study of the drug release behavior in acidic and basic media as well as the swelling ratio were achieved. The antibacterial activity and physical properties of all monomers and polymers were studied. [ABSTRACT FROM AUTHOR]