Department of Pharmaceutical Chemistry, Noida Institute of Engineering and Technology (Pharmacy Institute), Greater Noida 201310, India.
ANA Institute of Pharmaceutical Sciences and Research, Bareilly 243501, India.
Med Chem. 2023;19(4):325-360. doi: 10.2174/1573406418666220820110551.
Benzothiazole is a bicyclic heterocyclic compound that contains benzene fused with 1, 3- thiazole ring. Several researches established the potential of benzothiazoles as important moiety in various adverse pharmacological conditions. Benzothiazole and its derivatives have been in use and marketed as anti-microbial, anti-inflammatory, anti-diabetic, anti-oxidant, anti-convulsant, antitumor, etc. The variations in pharmacological potentials of benzothiazole and its derivatives have been rational with their chemical structure. Nowadays, hybridization of two or more pharmacophores to synthesize a single molecule with potent pharmacological action is used. This helps to synergize pharmacological properties, make interaction possible with many targets, or minimize the adverse effects associated with them. Several synthetic approaches have been reported for benzothiazole and its derivatives. In this present review article, we focused on recently adopted synthetic approaches for the synthesis of the benzothiazole nucleus and its derivatives. The structure-activity relationship in relation to different pharmacological activities has also been highlighted to provide a good understanding to the researchers for future research on benzothiazoles.
苯并噻唑是一种双环杂环化合物，其中包含苯与 1,3-噻唑环稠合。多项研究确立了苯并噻唑作为各种不良药理条件下重要部分的潜力。苯并噻唑及其衍生物已被用作和销售为抗菌、抗炎、抗糖尿病、抗氧化、抗惊厥、抗肿瘤等药物。苯并噻唑及其衍生物的药理潜力的变化与其化学结构有关。如今，将两个或多个药效团杂交合成具有强大药理作用的单一分子的方法被广泛应用。这有助于协同药理作用，使与许多靶点的相互作用成为可能，或最小化与之相关的不良反应。已经报道了几种苯并噻唑及其衍生物的合成方法。在本综述文章中，我们重点介绍了最近采用的苯并噻唑核及其衍生物的合成方法。还强调了与不同药理活性相关的结构-活性关系，以便为研究人员提供对苯并噻唑的未来研究的深入了解。
