THE SYNTHESIS AND EVALUATION OF CYCLIC UREAS AS HIV PROTEASE INHIBITORS - MODIFICATIONS OF THE P1 P1' RESIDUES/

Authors
PATEL M BACHELER LT RAYNER MM CORDOVA BC KLABE RM ERICKSONVIITANEN S SEITZ SP
Citation
M. Patel et al., THE SYNTHESIS AND EVALUATION OF CYCLIC UREAS AS HIV PROTEASE INHIBITORS - MODIFICATIONS OF THE P1 P1' RESIDUES/, Bioorganic & medicinal chemistry letters, 8(7), 1998, pp. 823-828
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
7
Year of publication
1998
Pages
823 - 828
Database
ISI
SICI code
0960-894X(1998)8:7<823:TSAEOC>2.0.ZU;2-5
Abstract
Two series of cyclic ureas modified at the P1/P1' residue were prepare d and evaluated for HIV protease inhibition and whole cell antiviral a ctivity. Compounds 8b, 10 (3- and 4-pyridylmethyl analogs) and 6b (4-m ethoxy analog) showed significant improvement in antiviral activity re lative to lead compounds DMP323 and DMP 450. (C) 1998 The DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd. All rights reserved.