Alzheimer is a neurodegenerative disease and requires the development of new scaffold to treat it. In this regard, thiazoles derivative are playing their significant role. In the current research paper we have focused our attention for the development of tetrasubstituted thiazole (3a-h) derivatives using domino synthesis by mixing the thiourea as a precursor, with acetophenone in the presence of iodine and tosic acid in DMSO and refluxed for 12–22 h. The structures of the newly synthesized compounds were confirmed by FTIR, ¹H NMR, ¹³C NMR and EIMS analysis. Thiazole derivatives were analyzed for their biological significances against acetyl and butylcholinesterase enzymes and compound 3b and 3d were found more active against these enzyme, respectively. The mode of inhibition was determined for the potent compounds against both the enzymes. Moreover, the molecular docking studies were carried out to explore the interactive behavior of the compounds within the active pocket of enzymes. Furthermore, the derivatives (3a-h) were evaluated for their anticancer potential against HeLa cancer cell lines. Most potent inhibition was observed by compound 3b.

阿尔茨海默氏症是一种神经退行性疾病，需要开发新的支架来治疗它。在这方面，噻唑衍生物发挥着重要作用。在当前的研究论文中，我们将注意力集中在使用多米诺骨牌合成的四取代噻唑（3a-h）衍生物的开发上，该合成是将硫脲作为前体与苯乙酮在DMSO中的碘和甲苯磺酸存在下回流12– 22小时 通过FTIR，¹ H NMR，¹³ C NMR和EIMS分析证实了新合成的化合物的结构。分析了噻唑衍生物对乙酰胆碱酯酶和丁基胆碱酯酶以及化合物3b和3d的生物学意义分别被发现对这些酶更具活性。确定了针对两种酶的有效化合物的抑制方式。此外，进行了分子对接研究以探索化合物在酶的活性口袋内的相互作用行为。此外，评估了衍生物（3a-h）对HeLa癌细胞系的抗癌潜力。化合物3b观察到了最有效的抑制作用。