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Journal of Chinese Pharmaceutical Sciences ›› 2020, Vol. 29 ›› Issue (2): 79-89.DOI: 10.5246/jcps.2020.02.006

• Review •     Next Articles

Pyridin-2(1H)-ones as HIV-1 NNRTIs: a combinatorial optimization strategy

Xixi Li, Qian Liu, Tao Sheng, Junyi Liu*, Xiaowei Wang*   

  1. Department of Chemical Biology, School of Pharmaceutical Sciences, State Key Laboratory of Natural and Biomimetic Drugs, Peking University Health Science Center, Beijing 100191, China
  • Received:2019-06-20 Revised:2019-10-17 Online:2020-02-29 Published:2019-11-15
  • Contact: Tel.:+86-10-82805203, E-mail: xiaoweiwang@bjmu.edu.cn
  • Supported by:
    National Natural Science Foundation of China (Grant No. 21172014, 20972011 and 21042009).

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

CLC Number: 

Supporting: