Author/Authors :
Philip E. J. Sanderson، نويسنده , , Matthew G. Stanton، نويسنده , , Bruce D. Dorsey، نويسنده , , Terry A. Lyle، نويسنده , , Colleen McDonough، نويسنده , , William M. Sanders، نويسنده , , Kelly L. Savage، نويسنده , , Adel M. Naylor-Olsen، نويسنده , , Julie A. Krueger، نويسنده , , S. Dale Lewis، نويسنده , , Bobby J. Lucas Jr.، نويسنده , , Joseph J. Lynch Jr.، نويسنده , , Youwei Yan، نويسنده ,
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.
