| Literature DB >> 12617893 |
Philip E J Sanderson1, Matthew G Stanton, Bruce D Dorsey, Terry A Lyle, Colleen McDonough, William M Sanders, Kelly L Savage, Adel M Naylor-Olsen, Julie A Krueger, S Dale Lewis, Bobby J Lucas, Joseph J Lynch, Youwei Yan.
Abstract
Starting from a 2-amino-6-methylpyridine P1 group and following a strategy of enlarging it whilst reducing its polarity, we have developed a series of potent, moderately basic azaindoles which are intrinsically much more selective for thrombin versus trypsin. Certain pyrazinone acetamide azaindole derivatives have pharmacokinetic parameters after oral administration to dogs, or efficacy in vitro, comparable to an optimized pyrazinone acetamide 2-amino-6-methylpyridine derivative.Entities:
Mesh：
Substances：
Year: 2003 PMID： 12617893 DOI： 10.1016/s0960-894x(03)00017-9
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823