The synthesis of a new series of S-substituted acetamides derivatives of 5-[(2-amino-1,3-thiazol-4-yl)methyl]-1,3,4-oxadiazol-2-thiol were synthesized and evaluated for enzyme inhibition study along with cytotoxic behavior. Ethyl 2-(2-amino-1,3-thiazol-4-yl)acetate was converted to corresponding acid hydrazide by hydrazine hydrate in ethanol. The reflux of acid hydrazide with carbon disulfide resulted to 5-[(2-amino-1,3-thiazol-4-yl)methyl]-1,3,4-oxadiazol-2-thiol. Different electrophiles were synthesized by the reaction of respective anilines (one in each reaction) and 2-bromoacetylbromide in an aqueous medium. The targeted bi-heterocyclic compounds were synthesized by stirring nucleophilic 5-[(2-amino-1,3-thiazol-4-yl)methyl]-1,3,4-oxadiazol-2-thiol with different acetamides electrophiles (one after another), in DMF using LiH as base and activator. The proposed structures of newly synthesized compounds were deduced by spectroscopic techniques such as 1H NMR, 13C NMR, EI MS and elemental analysis. These novel bi-heterocycles were tested for their anti-diabetic potential via the in vitro inhibition of $$\alpha $$ -glucosidase enzyme. The in silico study of these molecules was also coherent with their enzyme inhibition data. Furthermore, these molecules were analyzed for their cytotoxic behavior against brine shrimps. It was inferred from the results that most of them exhibited very potent inhibitory potential against the studied enzyme and can be utilized as valuable anti-diabetic agent.

中文翻译：

---

作为有价值的抗糖尿病药物的新型双杂环化合物的合成：2-({5-((2-Amino-1,3-Thiazol-4-yl)methyl)-1,3,4-Oxadiazol-2-yl}硫烷基)-N-(取代的)乙酰胺

合成了一系列新的 5-[(2-amino-1,3-thiazol-4-yl)methyl]-1,3,4-oxadiazol-2-thiol 的 S-取代乙酰胺衍生物并评价了酶抑制研究以及细胞毒性行为。2-(2-氨基-1,3-噻唑-4-基)乙酸乙酯在乙醇中通过水合肼转化为相应的酰肼。酰肼与二硫化碳的回流产生5-[(2-氨基-1,3-噻唑-4-基)甲基]-1,3,4-恶二唑-2-硫醇。不同的亲电子试剂是通过各自的苯胺（每个反应中一种）和 2-溴乙酰溴在水性介质中的反应合成的。通过将亲核 5-[(2-amino-1,3-thiazol-4-yl)methyl]-1,3,4-oxadiazol-2-thiol 与不同的乙酰胺亲电试剂（一个在其他），在 DMF 中使用 LiH 作为碱和活化剂。新合成化合物的结构是通过光谱技术如 1H NMR、13C NMR、EI MS 和元素分析推导出来的。通过体外抑制 $$\alpha $$ - 葡萄糖苷酶，测试了这些新型双杂环化合物的抗糖尿病潜力。这些分子的计算机研究也与它们的酶抑制数据一致。此外，还分析了这些分子对盐水虾的细胞毒性行为。从结果推断，它们中的大多数对所研究的酶表现出非常有效的抑制潜力，可用作有价值的抗糖尿病药物。通过体外抑制 $$\alpha $$ - 葡萄糖苷酶，测试了这些新型双杂环化合物的抗糖尿病潜力。这些分子的计算机研究也与它们的酶抑制数据一致。此外，还分析了这些分子对盐水虾的细胞毒性行为。从结果推断，它们中的大多数对所研究的酶表现出非常有效的抑制潜力，可用作有价值的抗糖尿病药物。通过体外抑制 $$\alpha $$ - 葡萄糖苷酶，测试了这些新型双杂环化合物的抗糖尿病潜力。这些分子的计算机研究也与它们的酶抑制数据一致。此外，还分析了这些分子对盐水虾的细胞毒性行为。从结果推断，它们中的大多数对所研究的酶表现出非常有效的抑制潜力，可用作有价值的抗糖尿病药物。