Tricyclic pharmacophore-based molecules as novel integrin α v β 3 antagonists. Part 1: Design and synthesis of a lead compound exhibiting α v β 3/α IIb β 3 dual …

…, M Ishikawa, M Yamamoto, S Murakami…

Index: Kubota, Dai; Ishikawa, Minoru; Yamamoto, Mikio; Murakami, Shoichi; Hachisu, Mitsugu; Katano, Kiyoaki; Ajito, Keiichi Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 7 p. 2089 - 2108

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Citation Number: 25

Abstract

In order to generate novel compounds with integrin αvβ3-antagonistic activity together with antiplatelet activity, tricyclic pharmacophore-based molecules were designed and synthesized. Although piperazine-containing compounds initially prepared were selective αIIbβ3 antagonists, replacement of piperazine with piperidine furnished a potent αvβ3/αIIbβ3 dual antagonist. Structure–activity relationship (SAR) studies provided clues for further ...