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Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold |
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| Authors: | Breslin Michael J Duggan Mark E Halczenko Wasyl Fernandez-Metzler Carmen Hunt Cecilia A Leu Chih-Tai Merkle Kara M Naylor-Olsen Adel M Prueksaritanont Thomayant Stump Gary Wallace Audrey Rodan Sevgi B Hutchinson John H |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA. john_hutchinson@merck.com |
| Abstract: | Two novel series of small-molecule RGD mimetics containing either a substituted pyridone or pyrazinone central constraint were prepared. Modification of the beta-alanine 3-substituent produced compounds that are potent and selective alpha(v)beta(3) antagonists and exhibit a range of physicochemical properties. |
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