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Recent Advances in the Design and Development of Non‐nucleoside Reverse Transcriptase Inhibitor Scaffolds
ChemMedChem ( IF 3.4 ) Pub Date : 2018-12-06 , DOI: 10.1002/cmdc.201800577
Pouria Shirvani 1 , Afshin Fassihi 1 , Lotfollah Saghaie 1
Affiliation  

Non‐nucleoside reverse transcriptase inhibitors (NNRTIs) have always been an important part of the anti‐HIV‐1 combination therapy known as combination antiretroviral therapy (cART) since 1996. The use of NNRTIs for about 22 years has led to some mutations in the residues that compose the reverse transcriptase active site, resulting in the emergence of drug‐resistant viruses. Thus, the search for new potent NNRTIs with an improved safety profile and activity against drug‐resistant HIV strains is indispensable, and many hit and lead NNRTIs have been discovered in the last decade. This review provides an overview of the development in this field from 2013 to August 2018.

中文翻译:

非核苷逆转录酶抑制剂支架设计和开发的最新进展

自1996年以来,非核苷类逆转录酶抑制剂(NNRTIs)一直是抗HIV-1联合疗法(称为联合抗逆转录病毒疗法(cART))的重要组成部分。NNRTIs的使用已约22年,导致其发生某些突变。组成逆转录酶活性位点的残基,导致耐药病毒的出现。因此,寻找具有增强的安全性和抗药性的HIV菌株活性的新的有效NNRTI必不可少,并且在过去十年中发现了许多流行和领先的NNRTI。这篇综述概述了2013年至2018年8月该领域的发展情况。
更新日期:2018-12-06
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