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Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements. |
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| Authors: | Paul J Coleman Karen M Brashear Cecilia A Hunt William F Hoffman John H Hutchinson Michael J Breslin Carol A McVean Ben C Askew George D Hartman Sevgi B Rodan Gideon A Rodan Chih Tai Leu Thomayant Prueksaritanont Carmen Fernandez-Metzler Bennett Ma Laura A Libby Kara M Merkle Gary L Stump Audrey A Wallace Joseph J Lynch Robert Lynch Mark E Duggan |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. paul_coleman@merck.com |
| Abstract: | Potent non-peptidic alpha(v)beta(3) antagonists have been prepared incorporating various beta-amino acids as aspartic acid mimetics. Modification of the beta-alanine 3-substituents alters the potency and physicochemical properties of these receptor antagonists and in some cases provides orally bioavailable alpha(v)beta(3) inhibitors. |
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