Synthesis and anti-HIV-1 activity of new delavirdine analogues carrying arylpyrrole moieties.
In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) values in the submicromolar range.
Pinna
G A
GA
Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, Sardinia, Italy. pinlab@uniss.it
Loriga
G
G
Murineddu
G
G
Grella
G
G
Mura
M
M
Vargiu
L
L
Murgioni
C
C
La Colla
P
P
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D020008:Delavirdine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical / Q000379:methods / Q000706:statistics & numerical data; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans
D019380:Anti-HIV Agents; D020008:Delavirdine