THE SYNTHESIS OF SYMMETRICAL AND UNSYMMETRICAL P1 P1' CYCLIC UREAS ASHIV PROTEASE INHIBITORS/

Authors
PATEL M KALTENBACH RF NUGIEL DA MCHUGH RJ JADHAV PK BACHELER LT CORDOVA BC KLABE RM ERICKSONVIITANEN S GARBER S REID C SEITZ SP
Citation
M. Patel et al., THE SYNTHESIS OF SYMMETRICAL AND UNSYMMETRICAL P1 P1' CYCLIC UREAS ASHIV PROTEASE INHIBITORS/, Bioorganic & medicinal chemistry letters, 8(9), 1998, pp. 1077-1082
Citations number
6
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
9
Year of publication
1998
Pages
1077 - 1082
Database
ISI
SICI code
0960-894X(1998)8:9<1077:TSOSAU>2.0.ZU;2-4
Abstract
Cyclic urea SD146, a potent HIV protease inhibitor bearing a flat resi stance profile, possessed poor solubility and bioavailability, which p recluded further development of the compound. In an effort to improve upon the pharmacokinetic profile of the compound, several analogs modi fied at the P1/P1' residues were prepared and evaluated. Several of th ose compounds displayed significant improvement of physical properties . (C) 1998 The DuPont Merck Pharmaceutical Company. Published by Elsev ier Science Ltd. All rights reserved.