Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.
Benzothiadiazine non-nucleoside reverse transcriptase inhibitors (NNRTIs) of HIV have been synthesized via a novel process to afford active inhibitors, with the most potent compound exhibiting an IC90 = 180 nM in a whole cell assay. The 2,2-dioxide-1H-2,1,3-benzothiadiazine ring system was constructed in one step from 2-amino-5-chlorobenzonitrile.
Corbett
J W
JW
DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA. jeffrey.w.corbett@dupontpharma.com
Gearhart
L A
LA
Ko
S S
SS
Rodgers
J D
JD
Cordova
B C
BC
Klabe
R M
RM
Erickson-Viitanen
S K
SK
D001581:Benzothiadiazines / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000201:enzymology; D006801:Humans; D015394:Molecular Structure; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
D001581:Benzothiadiazines; D018894:Reverse Transcriptase Inhibitors