Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001, India.
Vaish Institute of Pharmaceutical Education and Research, Rohtak, 124001, India.
Future Med Chem. 2023 Dec;15(24):2257-2268. doi: 10.4155/fmc-2023-0237. Epub 2023 Nov 20.
A new series of 3,5-disubstituted thiazolidin-2,4-dione molecules were derived and characterized using various spectral techniques (H NMR, IR, carbon, hydrogen, nitrogen, etc.) and physicochemical parameters. The molecules were derived using Knoevenagel condensation followed by Mannich reaction and further synthesized analogues were screened for their antioxidant and antimicrobial potential using 2,2-diphenyl-1-picrylhydrazyl free radical scavenging method and serial tube dilution method, respectively, along with studies (docking and absorption, distribution, metabolism and excretion parameters) to explore the drug-receptor interaction and druglikeness. In antimicrobial screening, the analogs , , and displayed promising activity while molecule exhibited better antioxidant potential in the series. In molecular docking analysis, the best-fitted analogs, namely, and , showed good interactions.
一系列 3,5-二取代噻唑烷-2,4-二酮分子被合成出来,并通过各种光谱技术(H NMR、IR、碳、氢、氮等)和物理化学参数进行了表征。这些分子是通过Knoevenagel 缩合、Mannich 反应得到的,进一步合成的类似物则通过 2,2-二苯基-1-苦基肼自由基清除法和连续管稀释法进行了抗氧化和抗菌活性筛选,同时还进行了(对接和吸收、分布、代谢和排泄参数)研究,以探索药物-受体相互作用和类药性。在抗菌筛选中,类似物 、 、 和 表现出了有前景的活性,而分子 则在该系列中表现出了更好的抗氧化潜力。在分子对接分析中,最佳拟合的类似物 、 ,表现出了良好的相互作用。