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.
Patel
M
M
DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA. mona.patel@dupontpharma.com
McHugh
R J
RJ
Cordova
B C
BC
Klabe
R M
RM
Erickson-Viitanen
S
S
Trainor
G L
GL
Rodgers
J D
JD
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