Anti human immunodeficiency virus-1 (HIV-1) agents 3. synthesis and in vitro anti-HIV-1 activity of some N-arylsulfonylindoles.
In order to find compounds with superior anti human immunodeficiency virus type 1 (HIV-1) activity, twelve simple N-arylsulfonylindoles (3a-l) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Several compounds demonstrated significant anti-HIV-1 activity, especially N-(3-nitrobenzene)sulfonyl-6-methylindole (3h) and N-(3-nitrobenzene)sulfonylindole (3i) showed the highest anti-HIV-1 activity with EC(50) values of 0.26 and 0.74 microg/ml, and TI values of 543.78 and >270.27, respectively.
Fan
Ling-Ling
LL
Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling, China.
Liu
Wu-Qing
WQ
Xu
Hui
H
Yang
Liu-Meng
LM
Lv
Min
M
Zheng
Yong-Tang
YT
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D007211:Indoles