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2000
Volume 14, Issue 3
  • ISSN: 1573-4064
  • E-ISSN: 1875-6638

Abstract

Background: The human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS) has always been a global health threat and leading cause of deaths. However, due to the emergence of drug-resistant HIV, an inevitable consequence of increasing use of antiretroviral drugs posed a major threat to antiretroviral therapy success. Objective: The discovery of anti-HIV-1 agents will be used for the effective treatment of HIV/AIDS. Method: In continuation of our program aimed to discover anti-HIV-1 agents, twelve matrine derivatives, such as 14-formyl-15-aryloxy/methoxymatrines (3a-j) and 14-aryloxymethylidenylmatrines (3k,l), were semi-prepared from matrine, and evaluated against HIV-1 replication in acutely infected C8166 cells in vitro. Results: Among them, compound 3j showed the most potent anti-HIV-1 activity with EC and therapeutic index (TI) values of 1.79 μg/mL, and 98.2, respectively. Conclusion: It has been demonstrated that the positions of methyl on the phenyl ring and 14- formylmatrine-15-oxy on the naphthyl ring were very important for the activity. It will lay the foundation for further structural modification and application of matrines as HIV-1 inhibitors.

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/content/journals/mc/10.2174/1573406413666171002120310
2018-05-01
2025-05-22
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  • Article Type:
    Research Article
Keyword(s): AIDS; antiretroviral drugs; HIV-1; inhibitors; Matrine derivatives; matrines; peptide drugs
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