|
|||||
|
|
Investigation of the terminal P4 domain in a series of D-phenylglycinamide-based factor Xa inhibitors |
|
| Authors: | Franciskovich Jeffry B Masters John J Weber Wayne W Klimkowski Valentine J Chouinard Michael Sipes Philip R Johnson Lea M Snyder David W Chastain Marcia K Craft Trelia J Towner Richard D Gifford-Moore Donetta S Froelich Larry L Smallwood Jeffrey K Foster Ronald S Smith Gerald F Liebeschuetz John W Murray Christopher W Young Stephen C |
| Affiliation: | Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. |
| Abstract: | Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant effects in vitro. A select subset containing various P1 indole constructs was further evaluated for their pharmacokinetic properties after oral administration to rats. |
| Keywords: | Factor Xa inhibitors d-Phenylgylcinamides Antithrombotics |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |