Bioorganic & Medicinal Chemistry Letters 2000-01-17

Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.

J W Corbett, L A Gearhart, S S Ko, J D Rodgers, B C Cordova, R M Klabe, S K Erickson-Viitanen

Index: Bioorg. Med. Chem. Lett. 10(2) , 193-5, (2000)

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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.