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Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists
William H Miller1, Peter J Manley, Russell D Cousins
1GlaxoSmithKline Pharmaceuticals, 1250 S. Collegeville Rd., PO Box 5089, PA 19426, USA. william_h_miller@gsk.com
Bioorganic & Medicinal Chemistry Letters
|April 2, 2003
Abstract:
In our continuing efforts to identify small molecule vitronectin receptor antagonists, we have discovered a series of phenylbutyrate derivatives, exemplified by 16, which have good potency and excellent oral bioavailability (approximately 100% in rats). This new series is derived conceptually from opening of the seven-membered ring of SB-265123.