Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Kanakapura, Ramanagaram, Bangalore 562112, India.
Department of Chemistry, Umeå University, 90187 Umeå, Sweden.
Eur J Med Chem. 2017 Sep 29;138:1002-1033. doi: 10.1016/j.ejmech.2017.07.038. Epub 2017 Jul 22.
Among sulfur containing heterocycles, benzothiophene and its derivatives are at the focus as these candidates have structural similarities with active compounds to develop new potent lead molecules in drug design. Benzo[b]thiophene scaffold is one of the privileged structures in drug discovery as this core exhibits various biological activities allowing them to act as anti-microbial, anti-cancer, anti-inflammatory, anti-oxidant, anti-tubercular, anti-diabetic, anti-convulsant agents and many more. Further, numerous benzothiophene-based compounds as clinical drugs have been extensively used to treat various types of diseases with high therapeutic potency, which has led to their extensive developments. Due to the wide range of biological activities of benzothiophene, their structure activity relationships (SAR) have generated interest among medicinal chemists, and this has culminated in the discovery of several lead molecules against numerous diseases. The present review is endeavoring to highlight the progress in the various pharmacological activities of benzo[b]thiophene derivatives. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic benzothiophene-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes. Also, SAR studies that highlight the chemical groups responsible for evoking the potential activities of benzothiophene derivatives are studied and compared.
在含硫杂环中，苯并噻吩及其衍生物是研究的重点，因为这些候选物与药物设计中开发新的有效先导分子的活性化合物具有结构相似性。苯并[b]噻吩结构是药物发现中的一种优势结构，因为这种核心表现出多种生物活性，使它们能够作为抗菌、抗癌、抗炎、抗氧化、抗结核、抗糖尿病、抗惊厥等药物。此外，许多基于苯并噻吩的化合物作为临床药物已被广泛用于治疗各种类型的疾病，具有很高的治疗效力，这导致了它们的广泛发展。由于苯并噻吩具有广泛的生物活性，其构效关系（SAR）引起了药物化学家的兴趣，这最终导致了针对许多疾病的几种先导分子的发现。本综述旨在强调苯并[b]噻吩衍生物的各种药理学活性的进展。希望本综述将有助于为更有效、毒性更低的基于苯并噻吩的药物的合理设计以及更有效的诊断剂和病理探针寻找提供新的思路。此外，还研究和比较了强调引起苯并噻吩衍生物潜在活性的化学基团的 SAR 研究。
