A simple and efficient protocol was developed to synthesize a new library of thiazolidine-4-one molecular hybrids (4a-n) via a one-pot multicomponent reaction involving 5-substituted phenyl-1,3,4-thiadiazol-2-amines, substituted benzaldehydes and 2-mercaptoacetic acid. The synthesized compounds were evaluated in vitro for their antidiabetic activities through α-glucosidase and α-amylase inhibition as well as their antioxidant and antimicrobial potentials. Compound 4e exhibited the most promising α-glucosidase and α-amylase inhibition with an IC₅₀ value of 2.59 μM, which is ~1.5- and 14-fold superior as compared to the standard inhibitor acarbose. Structure-activity relationship (SAR) analysis revealed that the nature and position of substituents on the phenyl rings had a significant effect on the inhibitory potency.

开发了一种简单有效的方案，通过涉及 5-取代苯基-1,3,4-噻二唑-2-胺的一锅多组分反应合成新的噻唑烷-4-one 分子杂化物 ( 4a-n )库，取代的苯甲醛和 2-巯基乙酸。通过抑制α-葡萄糖苷酶和α-淀粉酶以及它们的抗氧化和抗菌潜力，体外评估合成的化合物的抗糖尿病活性。化合物4e表现出最有希望的α-葡萄糖苷酶和α-淀粉酶抑制作用，IC ₅₀值为 2.59 μM，与标准抑制剂阿卡波糖相比，分别高出约 1.5 倍和 14 倍。构效关系（SAR）分析表明，苯环上取代基的性质和位置对抑制效力有显着影响。