Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics. |
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| Authors: | R M Keenan W H Miller L S Barton W E Bondinell R D Cousins D F Eppley S M Hwang C Kwon M A Lago T T Nguyen B R Smith I N Uzinskas C C Yuan |
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| Institution: | Research & Development Division, SmithKline Beecham Pharmaceuticals, Collegeville, PA 19426-0989, USA. |
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| Abstract: | 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. |
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