Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors

…, WM Sanders, KL Savage, AM Naylor-Olsen…

文献索引：Sanderson, Philip E. J.; Stanton, Matthew G.; Dorsey, Bruce D.; Lyle, Terry A.; McDonough, Colleen; Sanders, William M.; Savage, Kelly L.; Naylor-Olsen, Adel M.; Krueger, Julie A.; Lewis, S. Dale; Lucas, Bobby J.; Lynch, Joseph J.; Yan, Youwei Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 5 p. 795 - 798

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被引用次数: 25

摘要

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 ...