吡啶酮类HIV-1非核苷逆转录酶抑制剂: 组合优化设计策略

doi:10.5246/jcps.2020.02.006

摘要/Abstract

摘要：

随着艾滋病病毒在全球范围内的迅速传播和耐药性的日益严重, 开发新型有效的抗艾滋病药物显得尤为迫切。非核苷逆转录酶抑制剂(NNRTIs)以其结构多样性、独特的作用机制、高效低毒等特点, 成为对抗HIV感染最重要的抗逆转录病毒药物之一。吡啶酮衍生物作为NNRTIs的一种, 在近几十年的研究中取得了令人瞩目的成果。在这篇综述中, 我们概述了当前药物设计和药物化学方面的研究, 为发展下一代吡啶酮类HIV-1 NNRTIs提供思路。

关键词: HIV1-1, 逆转录酶, 耐药性, 非核苷类逆转录酶抑制剂, 吡啶酮衍生物

Abstract:

With rapid spread of HIV (human immunodeficiency virus) on a global scale and increasingly severe drug-resistance of it, it is urgently necessary to develop novel effective anti-HIV drugs. Non-nucleoside reverse transcriptase inhibitor (NNRTIs) is one of the most significant antiretroviral drugs for fighting against HIV infection due to their various structures, unique mode of action, good efficacy and low toxicity. Pyridinone derivatives, a type of NNRTIs, have been reported to achieve remarkable development in the past few decades. In this review, we summarized current drug design and medicinal chemistry efforts toward the development of next-generation pyridinones as HIV-1 NNRTIs.

Key words: HIV-1, Reverse transcriptase, Drug-resistance, NNRTIs, Pyridinone derivatives

中图分类号:

R914

Supporting:

李茜茜, 刘乾, 盛涛, 刘俊义, 王孝伟. 吡啶酮类HIV-1非核苷逆转录酶抑制剂: 组合优化设计策略[J]. 中国药学(英文版), 2020, 29(2): 79-89.

Xixi Li, Qian Liu, Tao Sheng, Junyi Liu, Xiaowei Wang. Pyridin-2(1H)-ones as HIV-1 NNRTIs: a combinatorial optimization strategy[J]. Journal of Chinese Pharmaceutical Sciences, 2020, 29(2): 79-89.

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