Artigo Acesso aberto Revisado por pares

Betulinic Acid Derivatives as Human Immunodeficiency Virus Type 2 (HIV-2) Inhibitors

2009; American Chemical Society; Volume: 52; Issue: 23 Linguagem: Inglês

10.1021/jm9004253

ISSN

1520-4804

Autores

Zhao Dang, Weihong Lai, Keduo Qian, Phong Ho, Kuo‐Hsiung Lee, Chin‐Ho Chen, Li Huang,

Tópico(s)

HIV Research and Treatment

Resumo

We previously reported that [[N-[3β-hydroxyllup-20(29)-en-28-oyl]-7-aminoheptyl]carbamoyl]methane (A43D, 4) was a potent HIV-1 entry inhibitor. However, 4 was inactive against HIV-2 virus, suggesting the structural requirements for targeting these two retroviruses are different. In this study, a series of new betulinic acid derivatives were synthesized, and some of them displayed selective anti-HIV-2 activity at nanomolar concentrations. In comparison to compounds with anti-HIV-1 activity, a shorter C-28 side chain is required for optimal anti-HIV-2 activity.

Referência(s)