Anti HIV-1 agents 5: synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro.
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.
Ran
Jun-Qiang
JQ
Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling, China.
Huang
Ning
N
Xu
Hui
H
Yang
Liu-Meng
LM
Lv
Min
M
Zheng
Yong-Tang
YT
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D007211:Indoles; C531932:3-acetylindole