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Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics
Paul J Coleman1, Ben C Askew, John H Hutchinson
1Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. paul_coleman@merck.com
Bioorganic & Medicinal Chemistry Letters
|August 6, 2002
Abstract:
Potent non-peptidic alpha(v)beta(3) antagonists have been prepared where deletion of an amide bond from an earlier series of linear RGD-mimetics provides a novel series of chain-shortened alpha(v)beta(3) antagonists with significantly improved oral pharmacokinetics. These chain-shortened alpha(v)beta(3) antagonists represent structurally novel integrin inhibitors.