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Anti HIV-1 agents 5: synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro.

Abstract：

:In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among of all the analogs, several compounds exhibited significant anti-HIV-1 activity, especially N-phenylsulfonyl-3-acetyl-6-methylindole (2j) and N-(p-ethyl)phenylsulfonyl-3-acetyl-6-methylindole (2n) showed the most potent anti-HIV-1 activity with EC(50) values of 0.36 and 0.13 microg/mL, and TI values of >555.55 and 791.85, respectively. It demonstrated that introduction of the acetyl group at the 3-position of N-arylsulfonyl-6-methylindoles could generally lead to the more potent analogs.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ran JQ,Huang N,Xu H,Yang LM,Lv M,Zheng YT

doi

10.1016/j.bmcl.2010.04.132

subject

Has Abstract

pub_date

2010-06-15 00:00:00

pages

3534-6

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00610-4

journal_volume

20

pub_type

杂志文章

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