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在药物发现中,1,2,3-三唑“一体化”环系统:良好的生物等排体、良好的药效团、良好的连接子和多功能的合成工具。

The 1,2,3-triazole 'all-in-one' ring system in drug discovery: a good bioisostere, a good pharmacophore, a good linker, and a versatile synthetic tool.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey.

Department of Analytical Chemistry, Faculty of Pharmacy, Mersin University, Mersin, Turkey.

出版信息

Expert Opin Drug Discov. 2022 Nov;17(11):1209-1236. doi: 10.1080/17460441.2022.2129613. Epub 2022 Oct 5.

DOI:10.1080/17460441.2022.2129613
PMID:36164263
Abstract

INTRODUCTION

The 1,2,3-triazole ring occupies an important space in medicinal chemistry due to its unique structural properties, synthetic versatility and pharmacological potential making it a critical scaffold. Since it is readily available through click chemistry for creating compound collections against various diseases, it has become an emerging area of interest for medicinal chemists.

AREAS COVERED

This review article addresses the unique properties of the1,2,3-triazole nucleus as an intriguing ring system in drug discovery while focusing on the most recent medicinal chemistry strategies exploited for the design and development of 1,2,3-triazole analogs as inhibitors of various biological targets.

EXPERT OPINION

Evidently, the 1,2,3-triazole ring with unique structural features has enormous potential in drug design against various diseases as a pharmacophore, a bioisoster or a structural platform. The most recent evidence indicates that it may be more emerging in drug molecules in near future along with an increasing understanding of its prominent roles in drug structures. The synthetic feasibility and versatility of triazole chemistry make it certainly ideal for creating compound libraries for more constructive structure-activity relationship studies. However, more comparative and target-specific studies are needed to gain a deeper understanding of the roles of the 1,2,3-triazole ring in molecular recognition.[Figure: see text].

摘要

简介

由于其独特的结构性质、合成多功能性和药理学潜力,1,2,3-三唑环在药物化学中占据着重要的地位,它是一个关键的支架。由于它可以通过点击化学轻松获得,用于针对各种疾病的化合物库的构建,因此它已成为药物化学家关注的新兴领域。

涵盖领域

本文讨论了 1,2,3-三唑核作为药物发现中引人入胜的环系统的独特性质,同时重点介绍了最近用于设计和开发 1,2,3-三唑类似物作为各种生物靶标抑制剂的药物化学策略。

专家意见

显然,具有独特结构特征的 1,2,3-三唑环作为药效团、生物等排体或结构平台,在针对各种疾病的药物设计中具有巨大的潜力。最近的证据表明,随着对其在药物结构中突出作用的认识不断增加,它在药物分子中可能会在不久的将来更加流行。三唑化学的合成可行性和多功能性使其非常适合用于创建化合物库,以进行更具建设性的构效关系研究。然而,需要进行更多的比较和针对特定目标的研究,以更深入地了解 1,2,3-三唑环在分子识别中的作用。[图:见正文]。

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