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Thiazole: A Review on Chemistry, Synthesis and Therapeutic Importance of its Derivatives.
Current Topics in Medicinal Chemistry ( IF 2.9 ) Pub Date : 2016-05-07 , DOI: 10.2174/1568026616666160506130731
Mahesh T Chhabria 1 , Shivani Patel , Palmi Modi , Pathik S Brahmkshatriya
Affiliation  

Thiazole, a unique heterocycle containing sulphur and nitrogen atoms, occupies an important place in medicinal chemistry. It is an essential core scaffold present in many natural (Vitamin B1- Thiamine) and synthetic medicinally important compounds. The versatility of thiazole nucleus demonstrated by the fact that it is an essential part of penicillin nucleus and some of its derivatives which have shown antimicrobial (sulfazole), antiretroviral (ritonavir), antifungal (abafungin), antihistaminic and antithyroid activities. The synthetic importance of thiazole derivatives, its reduced forms and condensed derivatives have been increased much by their recent applications as anticancer (tiazofurin), anthelmintic, vulcanising accelerators (mercaptobenzothiazole) and photographic sensitizers. Thiazole chemistry has developed steadily after the pioneering work of Hofmann and Hantsch. Bogert and co-workers made significant contribution to expand this field. Mills established the importance of thiazole ring in cyanine dyes which is used as photographic sensitizer. Benzothiazole, a fused derivative of thiazole have also proved its commercial value. Present review describes chemical and biological importance of thiazole and its condensed derivatives with an emphasis on recent developments.

中文翻译:

噻唑:其衍生物的化学,合成和治疗重要性的评论。

噻唑是一种独特的含有硫和氮原子的杂环,在药物化学中占有重要地位。它是存在于许多天然(维生素B1-硫胺素)和合成医学上重要化合物中的必不可少的核心支架。噻唑核是青霉素核及其某些衍生物的重要组成部分,证明了噻唑核的多功能性,这些衍生物已显示出抗菌剂(磺胺类),抗逆转录病毒剂(利托那韦),抗真菌剂(阿巴芬净),抗组胺和抗甲状腺活性。噻唑衍生物,其还原形式和缩合衍生物的合成重要性因其最近作为抗癌药(噻唑呋林),驱虫药,硫化促进剂(巯基苯并噻唑)和照相增敏剂的应用而大大增加。在霍夫曼和汉斯的开创性工作之后,噻唑化学发展稳定。博格特及其同事为扩展该领域做出了重大贡献。Mills确立了噻唑环在花青染料(用作感光剂)中的重要性。噻唑的稠合衍生物苯并噻唑也已证明其商业价值。本综述描述了噻唑及其缩合衍生物的化学和生物学重要性,并着重介绍了最新进展。
更新日期:2019-11-01
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