THE DE-NOVO DESIGN AND SYNTHESIS OF CYCLIC UREA INHIBITORS OF FACTOR XA - INITIAL SAR STUDIES

Authors
GALEMMO RA MADUSKUIE TP DOMINGUEZ C ROSSI KA KNABB RM WEXLER RR STOUTEN PFW
Citation
Ra. Galemmo et al., THE DE-NOVO DESIGN AND SYNTHESIS OF CYCLIC UREA INHIBITORS OF FACTOR XA - INITIAL SAR STUDIES, Bioorganic & medicinal chemistry letters, 8(19), 1998, pp. 2705-2710
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
19
Year of publication
1998
Pages
2705 - 2710
Database
ISI
SICI code
0960-894X(1998)8:19<2705:TDDASO>2.0.ZU;2-W
Abstract
In this report we discuss the design, synthesis, rind validation of a novel series of cyclic urea inhibitors of the blood coagulation protei n Factor Xa. This work culminates in compound 11, a mono-amidine inhib itor of fXa employing a new S4 ligand that reduces the cationic charac ter of these analogs. Compound 11 represents a lead for a series of mo re potent and selective inhibitors. (C) 1998 The DuPont Merck Pharmace utical Company. Published by Elsevier Science Ltd. All rights reserved .