Laboratory of Pharmacology and Toxicology, Biopharmaceutical and Toxicological Analysis Research Team, Faculty of Medicine and Pharmacy, Mohammed V University, Rabat, Morocco.
Laboratory of Medicinal Chemistry, Drug Sciences Research Center, Faculty of Medicine and Pharmacy, Mohammed V University in Rabat, Rabat, Morocco.
J Biomol Struct Dyn. 2024 Aug;42(13):6711-6725. doi: 10.1080/07391102.2023.2246574. Epub 2023 Aug 15.
The organic compounds 2-chloro--(aryl)acetamide and 2-azido--(aryl)acetamide were synthesized and analyzed using H, C NMR. The acute oral toxicity study was carried out according to OECD guidelines, which approve that the compounds (Ps18 and 153) were nontoxic. In addition, the compounds were evaluated for its antidiabetic and antihyperglycemic properties ( and ) and for antioxidant activity by utilizing several tests as 1,1-diphenyl2-picrylhydrazyl , (2,2'-azino-bis(3-ethyl benzthiazoline-6-sulfonicacid) , reducing power test and hydrogen peroxide activity . The molecular docking studies were performed to investigate the antidiabetic activity of Ps18 and 153 and compared with the experimental results. These compounds are a potent antidiabetic from both the experimental and molecular docking results. Finally, the physicochemical, pharmacokinetic and toxicological properties of Ps18 and 153 have been evaluated by using absorption, distribution, metabolism, excretion and toxicity analysis prediction.Communicated by Ramaswamy H. Sarma.
采用 H、C NMR 对 2-氯--（芳基）乙酰胺和 2-叠氮--（芳基）乙酰胺这两种有机化合物进行了合成和分析。根据经合组织（OECD）指南进行了急性口服毒性研究，该指南批准这两种化合物（Ps18 和 153）无毒。此外，还通过利用几种测试方法，如 1,1-二苯基 2-苦基肼基（1,1-diphenyl2-picrylhydrazyl，DPPH）、（2,2'- 联氮-双（3-乙基苯并噻唑啉-6-磺酸）（2,2'-azino-bis(3-ethyl benzthiazoline-6-sulfonicacid），还原能力测试和过氧化氢活性，评估了这些化合物的抗糖尿病和降血糖特性（和）以及抗氧化活性。进行了分子对接研究，以研究 Ps18 和 153 的抗糖尿病活性，并将其与实验结果进行比较。这些化合物在实验和分子对接结果中均表现出很强的抗糖尿病活性。最后，通过吸收、分布、代谢、排泄和毒性分析预测，对 Ps18 和 153 的物理化学、药代动力学和毒理学特性进行了评估。Ramaswamy H. Sarma 通讯。
