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A new hydroxyethylamine class of HIV-1 protease inhibitors with high antiviral potency and oral bioavailability

✍ Scribed by B.Moon Kim; Joseph P. Vacca; James P. Guare; Colleen M. Hanifin; Stuart R. Michelson; PaulL. Darke; Joan A. Zugay; Emilio A. Emini; William Schleif; Jiunn H. Lin; I-Wu Chen; Kari Vastag; Drazen Ostovic; Paul S. Anderson; Joel R. Huff

Book ID: 103982802
Publisher: Elsevier Science
Year: 1994
Tongue: English
Weight: 463 KB
Volume: 4
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(94)85024-0

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✦ Synopsis

A new hydroxyethylamine class of inhibitors was designed combining features from our clinical candidate, L-735.524, along with small heterocvclic PGaands develoDed in these laboratories. Hiahlv notent inhibitors possessing sub&omolar IC5O's have beenid&ified, whi<h exhibit good antiviral pott& h cell culture. L-738,872, a representative inhibitor in this class, showed 34% oral bioavailability in dogs.

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