Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors.

Abstract:

:We previously reported that [[N-[3beta-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.

journal_name

J Med Chem

authors

Dang Z,Lai W,Qian K,Ho P,Lee KH,Chen CH,Huang L

doi

10.1021/jm9004253

subject

Has Abstract

pub_date

2009-12-10 00:00:00

pages

7887-91

issue

23

eissn

0022-2623

issn

1520-4804

journal_volume

52

pub_type

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