title: Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.
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.
authors.affiliation: DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA. jeffrey.w.corbett@dupontpharma.com
authors.forename: J W
authors.initials: JW
authors.lastname: Corbett
authors.forename: L A
authors.initials: LA
authors.lastname: Gearhart
authors.forename: S S
authors.initials: SS
authors.lastname: Ko
authors.forename: J D
authors.initials: JD
authors.lastname: Rodgers
authors.forename: B C
authors.initials: BC
authors.lastname: Cordova
authors.forename: R M
authors.initials: RM
authors.lastname: Klabe
authors.forename: S K
authors.initials: SK
authors.lastname: Erickson-Viitanen
mesh_terms: 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
chemical_list: D001581:Benzothiadiazines; D018894:Reverse Transcriptase Inhibitors