Add time:08/04/2019 Source:sciencedirect.com
Dihydropyran-2-one possessing a sulfamate moiety at the 4-position of the thiophenyl ring were designed to reach S3′ pocket of the HIV protease. Synthetic routes for the preparation of thiotosylates possessing 3-(2-t-butyl-5-methyl-4-sulfamate) phenylthio moiety were established. SAR of various sulfamate analogs including HIV protease binding affinities, antiviral activities and therapeutic indices will be described.
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