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 …
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 ...
