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Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.
Hoekstra WJ, Maryanoff BE, Damiano BP, Andrade-Gordon P, Cohen JH, Costanzo MJ, Haertlein BJ, Hecker LR, Hulshizer BL, Kauffman JA, Keane P, McComsey DF, Mitchell JA, Scott L, Shah RD, Yabut SC. Hoekstra WJ, et al. Among authors: haertlein bj. J Med Chem. 1999 Dec 16;42(25):5254-65. doi: 10.1021/jm990418b. J Med Chem. 1999. PMID: 10602710
In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
Costanzo MJ, Almond HR Jr, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE. Costanzo MJ, et al. Among authors: haertlein bj. J Med Chem. 2005 Mar 24;48(6):1984-2008. doi: 10.1021/jm0303857. J Med Chem. 2005. PMID: 15771442
21 results