Kamal Ahmed, Syed Mohammed Ali Hussaini, Mohammed Shaheer Malik
CSIR-Indian Institute of Chemical Technology, Medicinal Chemistry and Pharmacology , Hyderabad- 500007 , India +91 40 27193157 ; +91 40 27193189 ;
Expert Opin Ther Pat. 2015 Mar;25(3):335-49. doi: 10.1517/13543776.2014.999764. Epub 2015 Jan 12.
Benzothiazole is a versatile fused heterocyclic scaffold with extensive pharmaceutical applications. Several benzothiazole derivatives possess broad spectrum of antimicrobial, analgesic, anti-inflammatory, antidiabetic activities and so on, and the structurally simple 2-arylbenzothiazoles are potential antitumor agents. Some of the compounds containing benzothiazole ring system are in clinical usage for the treatment of various diseases/disorders.
In the present review, the authors summarize inventions carried out towards the development of benzothiazole-based chemotherapeutic agents. It provides an overview of the patents filed during 2010 - 2014 pertaining to the anticancer, antimicrobial, anti-inflammatory and other biological activities of benzothiazole derivatives.
Several molecules containing benzothiazole skeleton are agents of choice for the treatment of various human diseases/disorders. Its versatile character of being capable of serving as ligand to various biomolecules attracted the interest of medicinal chemists for the development of therapies for respective ailments, especially, the 2-arylbenzothiazole moiety which is under development for the treatment of cancer. This signifies the increasing importance of benzothiazole nucleus in the area of drug discovery. Its structural simplicity and ease of synthesis provides scope for the development of chemical libraries that could serve in the discovery of new chemical entities progressing towards the market.
苯并噻唑是一种用途广泛的稠合杂环骨架,具有广泛的药物应用。几种苯并噻唑衍生物具有广谱抗菌、止痛、抗炎、抗糖尿病等活性,结构简单的2-芳基苯并噻唑是潜在的抗肿瘤药物。一些含有苯并噻唑环系统的化合物正在临床上用于治疗各种疾病/病症。
在本综述中,作者总结了为开发基于苯并噻唑的化学治疗剂所进行的发明。它概述了2010年至2014年期间提交的与苯并噻唑衍生物的抗癌、抗菌、抗炎和其他生物活性相关的专利。
几种含有苯并噻唑骨架的分子是治疗各种人类疾病/病症的首选药物。其作为各种生物分子配体的多功能特性吸引了药物化学家对开发针对各自疾病的疗法的兴趣,特别是正在开发用于治疗癌症的2-芳基苯并噻唑部分。这表明苯并噻唑核在药物发现领域的重要性日益增加。其结构简单且易于合成,为开发可用于发现向市场推进的新化学实体的化学文库提供了空间。