Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics

Article abstract of DOI:10.1016/S0960-894X(99)00282-6

A peptide RGD analog containing a novel 2-aminopyridine arginine mimetic was discovered to have good affinity and selectivity for the vitronectin receptor. Incorporation of the 2-aminopyridine arginine mimetic into the 3- oxo-1,4-benzodiazepine-2-acetic acid integrin antagonist series led to novel and potent nonpeptide vitronectin receptor antagonists with promising levels of oral bioavailability.