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

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review.
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DOI:
10.1039/c9ra09510a
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发表时间:
2020-02-04
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影响因子:
3.9
通讯作者:
--
中科院分区:
化学3区
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该综述强调了通过 CuAAC 反应合成的 1,2,3-三唑作为抗菌、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力。点击化学的重要性在于其“更快”的方法,能够从简单且廉价的起始材料中生产出具有高产率和纯度的复杂而高效的药物。考虑到针对不同微生物种类的 MIC、IC50 和 EC50 值,编制了不同三唑基化合物的活性。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。该综述强调了通过 CuAAC 反应合成的 1,2,3-三唑作为抗菌、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力。
The review lays emphasis on the significance of 1,2,3-triazoles synthesized via 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, IC50, and EC50 values against different species of microbes. In addition to this, the anti-oxidant property of triazolyl compounds have also been reviewed and discussed. The review lays emphasis on the significance of 1,2,3-triazoles synthesized via CuAAC reaction having potential to act as anti-microbial, anti-cancer, anti-viral, anti-inflammatory, anti-tuberculosis, anti-diabetic, and anti-Alzheimer drugs.
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