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Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors
J W Corbett1, L A Gearhart, S S Ko
1DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA. jeffrey.w.corbett@dupontpharma.com
Bioorganic & Medicinal Chemistry Letters
|February 15, 2000
Abstract:
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.