Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action

RE Olson, TM Sielecki, J Wityak, DJ Pinto…

Index: Olson, Richard E.; Sielecki, Thais M.; Wityak, John; Pinto, Donald J.; Batt, Douglas G.; Frietze, William E.; Liu, Jie; Tobin, A. Ewa; Orwat, Michael J.; Di Meo, Susan V.; Houghton, Gregory C.; Lalka, George K.; Mousa, Shaker A.; Racanelli, Adrienne L.; Hausner, Elizabeth A.; Kapil, Ram P.; Rabel, Shelley R.; Thoolen, Martin J.; Reilly, Thomas M.; Anderson, Paul S.; Wexler, Ruth R. Journal of Medicinal Chemistry, 1999 , vol. 42, # 7 p. 1178 - 1192

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Citation Number: 48

Abstract

Modification of the α-carbamate substituent of isoxazoline GPIIb/IIIa (αIIbβ3) antagonist DMP 754 (7) led to a series of α-sulfonamide and α-sulfamide diaminopropionate isoxazolinylacetamides which were found to be potent inhibitors of in vitro platelet aggregation. Aryl-and heteroaryl-α-sulfonamide groups, in conjunction with (5 R)- isoxazoline (2 S)-diaminopropionate stereochemistry, were found to impart a pronounced ...