Anti human immunodeficiency virus type 1 (HIV-1) agents 4. Discovery of 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates as new HIV-1 inhibitors in vitro.
To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates (4a-j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline p-ethylbenzenesulfonate (4g) and 5,5'-(p-phenylenebisazo)-8-hydroxyquinoline p-chlorobenzenesulfonate (4i) showed the more potent anti-HIV-1 activity with 50% effective concentration (EC(50)) values of 2.59 and 4.01 microg/ml, and therapeutic index (TI) values of 31.77 and 24.51, respectively.
Zeng
Xi-Wen
XW
Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling, China.
Huang
Ning
N
Xu
Hui
H
Yang
Wen-Bin
WB
Yang
Liu-Meng
LM
Qu
Huan
H
Zheng
Yong-Tang
YT
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D055808:Drug Discovery; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D006912:Hydroxyquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D006912:Hydroxyquinolines