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An oxidative amidation of 2-methylpyridines/2-methylbenzimidazole with amines using copper acetate and elemental sulfur in DMSO to afford various -(hetero)arylamides has been accomplished. Mechanistic studies reveal the intermediacy of -(pyridin-2-ylmethyl)aniline and confirm the role of DMSO as the oxygen source.
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http://dx.doi.org/10.1039/d2ob01106a | DOI Listing |
Arch Pharm (Weinheim)
September 2025
Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Nitazoxanide (NTZ), an FDA-approved drug, served as the framework for synthesizing 22 new broad-spectrum antimicrobial agents from 4-aminosalicylic acid via protection-deprotection, Staudinger reduction, Clauson-Kaas pyrrole synthesis, and nucleophilic substitution. These compounds were evaluated for antibacterial, antimycobacterial, and antitrypanosomal activities. Several compounds, particularly 10, 11, 13, and 22, surpassed the antibacterial activity of NTZ and its active metabolite tizoxanide (TIZ) against all tested pathogens, with MICs ranging from 1.
View Article and Find Full Text PDFFood Res Int
November 2025
State Key Laboratory of Food Science and Resources, Jiangnan University, Wuxi 214122, Jiangsu, China.
Cognitive disorders, a rapidly growing public health concern, can be prevented by a healthy diet. Several studies have shown that protein intake is a key modulator of cognitive function. The development of precision nutrition has allowed the study of specific amino acids within proteins, with many studies reporting that the level of methionine (Met) intake plays a central role in modulating cognitive function.
View Article and Find Full Text PDFJ Org Chem
September 2025
School of Chemistry and Chemical Engineering, Zhejiang Sci-Tech University, Hangzhou 310018, China.
A palladium-catalyzed cyclization and carbonylation of -propargylamides with amines has been developed, which incorporates an amide unit into 3,4-dihydroisoquinolin-1(2)-one scaffolds. By using benzene-1,3,5-triyl triformate (TFBen) as the safe and convenient CO source, the reaction proceeded smoothly to afford a variety of amide-containing 3,4-dihydroisoquinolin-1(2)-one derivatives in high yields.
View Article and Find Full Text PDFJMIR Diabetes
August 2025
1. Division of Endocrinology, Metabolism and Diabetes, Department of Internal Medicine, Fatmawati General Hospital, Jakarta, Indonesia, Jl. RS. Fatmawati Raya, Cilandak Bar., Kec. Cilandak, South Jakarta, ID.
Background: Insulin therapy is crucial for type 2 diabetes mellitus management, with increasing usage in Indonesia, and its effectiveness is well-established. However, prescribing insulin poses various challenges that can impact the effectiveness of insulin. Patient education is crucial for the successful implementation of insulin therapy.
View Article and Find Full Text PDFOrg Lett
September 2025
Engineering Research Center of Photoenergy Utilization for Pollution Control and Carbon Reduction, State Key Laboratory of Green Pesticide, International Joint Research Center for Intelligent Biosensing Technology and Health, College of Chemistry, Central China Normal University, Wuhan, Hubei 430079
Structurally diverse 1,2-sulfinate-sulfonate esters are shown to be conveniently prepared through visible light-induced sulfonation and sulfinylation of difunctionalized alkenes using alcohols and NaHSO. The reactions proceed under mild conditions in the presence of photocatalysts and HCOH as an additive, exhibiting good functional group tolerance and a broad scope. Furthermore, this method is scalable and has been successfully applied to synthesize 1,2-disulfonic acid esters.
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