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Article

2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.

Journal of medicinal chemistry - 8 Apr 2021

Kang Dongwei, Ruiz Francesc X, Sun Yanying, Feng Da, Jing Lanlan, Wang Zhao, Zhang Tao, Gao Shenghua, Sun Lin, De Clercq Erik, Pannecouque Christophe, Arnold Eddy, Zhan Peng, Liu Xinyong

Abstract excerpt

There is an urgent unmet medical need for novel human immunodeficiency virus type 1 (HIV-1) inhibitors that are effective against a variety of NNRTI-resistance mutations. We report our research efforts aimed at discovering a novel chemotype of anti-HIV-1 agents with improved potency against a variety of NNRTI-resistance mutations in this paper. Structural modifications of the lead K-5a2 led to the identification...

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Anti-HIV Agents
Crystallography, X-Ray
Drug Design
HIV Reverse Transcriptase
Molecular Structure

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Rats, Sprague-Dawley

Reverse Transcriptase Inhibitors

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Identifiers

PMID: 33734714
DOI: 10.1021/acs.jmedchem.1c00268
PMCID: PMC8594587

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