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1,3-噻唑核心结构在新型先导化合物鉴定和药物发现中的最新应用。

Recent applications of 1,3-thiazole core structure in the identification of new lead compounds and drug discovery.

作者信息

Ayati Adile, Emami Saeed, Asadipour Ali, Shafiee Abbas, Foroumadi Alireza

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.

Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

出版信息

Eur J Med Chem. 2015 Jun 5;97:699-718. doi: 10.1016/j.ejmech.2015.04.015. Epub 2015 Apr 13.

DOI:10.1016/j.ejmech.2015.04.015
PMID:25934508
Abstract

1,3-Thiazole is one of the most important scaffolds in heterocyclic chemistry and drug design and discovery. It is widely found in diverse pharmacologically active substances and in some naturally-occurring compounds. Thiazole is a versatile building-block for lead generation, and is easily access of diverse derivatives for subsequent lead optimization. In the recent years, many thiazole derivatives have been synthesized and subjected to varied biological activities. In this article we intended to review the most important biological effects of thiazole-based compounds and highlight their roles in new leads identification and drug discovery. This article is also intended to help researches for finding potential future directions on the development of more potent and specific analogs of thiazole-based compounds for various biological targets.

摘要

1,3-噻唑是杂环化学以及药物设计与发现领域中最重要的骨架之一。它广泛存在于多种具有药理活性的物质以及一些天然化合物中。噻唑是用于生成先导化合物的通用构建模块,并且易于获得各种衍生物以用于后续的先导化合物优化。近年来,许多噻唑衍生物已被合成并测试其各种生物活性。在本文中,我们旨在综述基于噻唑的化合物的最重要生物效应,并突出它们在新先导化合物识别和药物发现中的作用。本文还旨在帮助研究人员找到未来潜在的发展方向,以开发针对各种生物靶点的更有效、更具特异性的基于噻唑的化合物类似物。

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