Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina, USA.
Beijing Key Laboratory of New Drug Discovery based on Classic Chinese Medicine Prescription, Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.
Med Res Rev. 2020 Nov;40(6):2339-2385. doi: 10.1002/med.21708. Epub 2020 Jul 14.
The human immunodeficiency virus/acquired immunodeficiency syndrome (HIV/AIDS) epidemic is one of the world's most serious health challenges. Although combination antiretroviral therapy provides effective viral suppression, current medicines used against HIV cannot completely eradicate the infectious disease and often have associated toxicities and severe side effects in addition to causing drug resistance. Therefore, the continued development of new antiviral agents with diverse structures and novel mechanisms of action remains a vital need for the management of HIV/AIDS. Natural products are an important source of drug discovery, and certain triterpenes and their analogs have demonstrated potential as pharmaceutical precursors for the treatment of HIV. Over the past decade, natural triterpenoids and analogs have been extensively studied to find new anti-HIV drugs. This review discusses the anti-HIV triterpenoids and analogs reported during the period of 2009-2019. The article includes not only a comprehensive review of the recent anti-HIV agent development from the perspective of medicinal chemistry, but also discusses structure-activity relationship analyses of the described triterpenoids.
人类免疫缺陷病毒/获得性免疫缺陷综合征（HIV/AIDS）疫情是全球面临的最严重的健康挑战之一。尽管联合抗逆转录病毒疗法可提供有效的病毒抑制，但目前用于治疗 HIV 的药物并不能完全消除这种传染病，而且除了引起耐药性外，还常常具有相关毒性和严重的副作用。因此，继续开发具有不同结构和新颖作用机制的新型抗病毒药物仍然是管理 HIV/AIDS 的迫切需要。天然产物是药物发现的重要来源，某些三萜类化合物及其类似物已被证明是治疗 HIV 的药物前体有潜力。在过去的十年中，人们广泛研究了天然三萜类化合物及其类似物，以寻找新的抗 HIV 药物。本综述讨论了 2009-2019 年期间报道的抗 HIV 三萜类化合物及其类似物。本文不仅从药物化学的角度对最近的抗 HIV 药物开发进行了全面综述，还讨论了所描述的三萜类化合物的构效关系分析。
