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作为药物发现中药效基团的铜催化叠氮-炔环加成反应(CuAAC)组装的1,2,3-三唑连接的电子等排体:综述

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review.

作者信息

Rani Alisha, Singh Gurjaspreet, Singh Akshpreet, Maqbool Ubair, Kaur Gurpreet, Singh Jandeep

机构信息

Department of Chemistry, Lovely Professional University Phagwara-144411 Punjab India

Department of Chemistry, Centre of Advanced Studies in Chemistry, Panjab University Chandigarh-160014 India.

出版信息

RSC Adv. 2020 Feb 4;10(10):5610-5635. doi: 10.1039/c9ra09510a.

Abstract

The review lays emphasis on the significance of 1,2,3-triazoles synthesized CuAAC reaction having potential to act as anti-microbial, anti-cancer, anti-viral, anti-inflammatory, anti-tuberculosis, anti-diabetic, and anti-Alzheimer drugs. The importance of click chemistry is due to its 'quicker' methodology that has the capability to create complex and efficient drugs with high yield and purity from simple and cheap starting materials. The activity of different triazolyl compounds was compiled considering MIC, IC, and EC values against different species of microbes. In addition to this, the anti-oxidant property of triazolyl compounds have also been reviewed and discussed.

摘要

该综述强调了通过铜催化的叠氮-炔环加成(CuAAC)反应合成的1,2,3-三唑类化合物作为抗菌、抗癌、抗病毒、抗炎、抗结核、抗糖尿病和抗阿尔茨海默病药物的潜在意义。点击化学的重要性在于其“更快”的方法,该方法能够从简单且廉价的起始原料中高产率、高纯度地制备复杂而高效的药物。考虑到不同三唑基化合物对不同微生物物种的最低抑菌浓度(MIC)、半数抑制浓度(IC)和半数效应浓度(EC)值,对其活性进行了汇总。除此之外,还对三唑基化合物的抗氧化性能进行了综述和讨论。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac87/9049420/78ffdfe99fba/c9ra09510a-f1.jpg

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