Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

Wang Zhao; Cherukupalli Srinivasulu; Xie MinghuiWang WenboJiang XiangyiJia RuifangPannecouque ChristopheDe Clercq ErikKang DongweiZhan PengLiu Xinyong

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Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

机译：Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

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Currently, HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are a major component of the highly active anti-retroviral therapy (HAART) regimen. However, the occurrence of drug-resistant strains and adverse reactions after long-term usage have inevitably compromised the clinical application of NNRTIs. Therefore, the development of novel inhibitors with distinct anti-resistance profiles and better pharmacological properties is still an enormous challenge. Herein, we summarize state-of-the-art medicinal chemistry strategies for the discovery of potent NNRTIs, such as structure-based design strategies, contemporary computer-aided drug design, covalent-binding strategies, and the application of multi-target-directed ligands. The strategies described here will facilitate the identification of promising HIV-1 NNRTIs.

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来源
《Journal of Medicinal Chemistry》 |2022年第5期|3729-3757|共29页
作者
Wang Zhao; Cherukupalli Srinivasulu; Xie MinghuiWang WenboJiang XiangyiJia RuifangPannecouque ChristopheDe Clercq ErikKang DongweiZhan PengLiu Xinyong;
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Shandong Univ;

Katholieke Univ Leuven;

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正文语种英语
中图分类药学;
关键词
DAPIVIRINE VAGINAL RING; DESIGNED DUAL INHIBITORS; WILD-TYPE; DRUG-RESISTANCE; PICOMOLAR INHIBITORS; CRYSTAL-STRUCTURES; IMPROVED POTENCY; CONFORMATIONAL RESTRICTION; POSITIONAL ADAPTABILITY; ANTIVIRAL ACTIVITY;

Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

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