Title of article
Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
795
To page
798
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793017
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