Design, synthesis, and in vitro activities of benzamide-core glycoprotein IIb/IIIa antagonists: 2, 3-diaminopropionic acid derivatives as surrogates of aspartic acid

…, J Roderick, S Jackson, M Rafalski, A Rockwell…

Index: Xue, Chu-Biao; Roderick, John; Jackson, Sharon; Rafalski, Maria; Rockwell, Arlene; Mousa, Shaker; Olson, Richard E.; DeGrado, William F. Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 4 p. 693 - 705

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Citation Number: 26

Abstract

In an effort to discover novel nonpeptide glycoprotein IIb/IIIa (GPIIb/IIIa, αIIb/β3) inhibitors, we investigated RGD mimetics featuring a 3-substituted benzoic acid as the core, benzamidine as the basic moiety, and a series of β-and α-substituted β-alanine derivatives as aspartic acid surrogates. It was found that the use of β-methyl β-alanine slightly improved the anti- aggregant potency in human platelet-rich plasma over the unsubstituted β-alanine ...