Abstract

Heterocyclic compounds occupy a central position in synthetic organic chemistry due to their broad range of applications. The electron-rich sulfur atom of benzo[b]thiophenes with its planar structure enhances the binding affinity with various enzymes and receptors. Since it is a polar compound, it improves the pharmacokinetic features of the pilot molecules and it can thus be consequently used as an attractive probe due to low toxicity, high solubility, and bioavailability. This scaffold exhibits numerous biological activities such as anti-microbial, anti-cancer, anti-leishmanial, anti-oxidant, anti-malarial, anti-diabetic, anthelmintic, etc. The common methods used for their synthesis mainly include Lewis acid-catalyzed, halogen-catalyzed, transition metal-catalyzed, base-catalyzed, electrophilic, and acid-catalyzed cyclization reactions. This review examines diverse synthetic methods and biological applications of the reported benzo[b]thiophene derivatives.

摘要

由于其广泛的应用范围，杂环化合物在有机合成化学中占据中心地位。苯并[ b的富电子硫原子]具有平面结构的噻吩增强了与各种酶和受体的结合亲和力。由于它是一种极性化合物，它改善了试验分子的药代动力学特征，因此由于低毒性、高溶解度和生物利用度，它可以用作有吸引力的探针。该支架具有多种生物活性，如抗微生物、抗癌、抗利什曼原虫、抗氧化、抗疟疾、抗糖尿病、驱虫等。常用的合成方法主要有路易斯酸催化、卤素催化、过渡金属催化、碱催化、亲电和酸催化的环化反应。本综述考察了已报道的苯并[ b ]噻吩衍生物的多种合成方法和生物学应用。