Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.
A series of 3,3-disubstituted quinoxalinones was prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The N-allyl (6b and 6f), N-cyclopropylmethyl (6a, 6g, 6h, and 6k) and N-carboalkoxy (6m-6y) substituted compounds displayed activity comparable or better than Efavirenz and GW420867X.
DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA. mona.patel@dupontpharma.com
M
M
Patel
R J
RJ
McHugh
B C
BC
Cordova
R M
RM
Klabe
S
S
Erickson-Viitanen
G L
GL
Trainor
J D
JD
Rodgers
D004341:Drug Evaluation; D054303:HIV Reverse Transcriptase / Q000187:drug effects*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*
D011810:Quinoxalines; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase