Design of a new class of orally active fibrinogen receptor antagonists

SI Klein, BF Molino, M Czekaj, CJ Gardner…

文献索引：Klein, Scott I.; Molino, Bruce F.; Czekaj, Mark; Gardner, Charles J.; Chu, Valeria; Brown, Karen; Sabatino, Ralph D.; Bostwick, Jeffrey S.; Kasiewski, Charles; Bentley, Ross; Windisch, Vincent; Perrone, Mark; Dunwiddie, Christopher T.; Leadley, Robert J. Journal of Medicinal Chemistry, 1998 , vol. 41, # 14 p. 2492 - 2502

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被引用次数: 32

摘要

The integrin receptor recognition sequence Arg-Gly-Asp was successfully used as a template from which to develop a series of potent, selective, orally active, peptide-based fibrinogen receptor antagonists with a long duration of action. Simple modifications centered on the Arg and Gly residues quickly led to a modified peptide (1) with significantly enhanced ability to inhibit in vitro platelet aggregation. Substitution of the guanidino group in 1 by ...