Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors.
Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors.
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DOI:
10.1021/jm9004253
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发表时间:
2009-12-10
影响因子:
7.3
通讯作者:
Huang L
中科院分区:
文献类型:
--
作者:
Dang Z;Lai W;Qian K;Ho P;Lee KH;Chen CH;Huang L
We previously reported that [[N-[3β-hydroxyl-lup-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.
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