1.
Bioorg Med Chem Lett
; 11(2): 227-30, 2001 Jan 22.
Article
in English
| MEDLINE
| ID: mdl-11206465
ABSTRACT
Starting from the achiral and potent factor Xa inhibitor 1, a new and flexible solid-phase optimisation strategy is described to reduce its cationic character. By replacing one positively charged side chain by a lipophilic substituent, a novel series of highly potent and selective achiral factor Xa inhibitors was discovered. The identified lipophilic replacements in the S4 pocket might be valuable for other approaches towards fXa inhibitors.