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Synthesis, characterization and evaluation of new thiazole derivatives as anthelmintic agents
Indian Journal of Chemistry, Section B ( IF 0.456 ) Pub Date : 2021-04-15
Sai Krishna Guduru, D Kumaraswamy, K Sirisha, K Sai Santhoshi

A series of 2-amino substituted 4-phenyl thiazole derivatives has been synthesized by the conventional method. The thiazole derivatives have been synthesized by three steps. The obtained five derivatives have been purified by recrystallization process by using methanol as solvent and column chromatography [IVd Compound] and have been characterized by melting point, TLC, FTIR, 1H NMR and mass spectral data. All the five derivatives have been evaluated using in silico studies by using different softwares (Lipinski’s Rule of 5, OSIRIS molecular property explorer, Molsoft molecular property explorer, PASS and docking studies). These compounds have then been evaluated for anthelmintic activity against Indian adult earth worms (Pheretima postuma). All the compounds show significant anthelmintic activity. The compound IVc and IVe are shown to be potent compounds when compared with the standard drug (Mebendazole). Molecular docking studies have guided and prove the biological activity of the sythesised compounds against beta tubulin protein (1OJ0).

中文翻译:

新型噻唑类驱虫药的合成,表征和评价

通过常规方法已经合成了一系列2-氨基取代的4-苯基噻唑衍生物。噻唑衍生物已通过三个步骤合成。所获得的五种衍生物已经通过使用甲醇作为溶剂的重结晶工艺和柱色谱法[IVd化合物]进行了纯化,并通过熔点,TLC,FTIR,1 H NMR和质谱数据进行了表征。使用不同的软件(Lipinski's Rule of 5,OSIRIS分子特性浏览器,Molsoft分子特性浏览器,PASS和对接研究),通过计算机研究对所有五种衍生物进行了评估。然后评估了这些化合物对印度成虫的驱虫活性(Pheretima postuma)。所有化合物均显示出显着的驱虫活性。与标准药物(甲苯咪唑)相比,化合物IVc和IVe被证明是有效的化合物。分子对接研究已指导并证明了合成化合物对抗β微管蛋白(1OJ0)的生物活性。
更新日期:2021-04-15
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