Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors |
| |
Authors: | Heinelt U Herok S Matter H Wildgoose P |
| |
Institution: | Aventis Pharma, Frankfurt, Germany. uwe.heinelt@aventis.com |
| |
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. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |