Piperidine-containing β-arylpropionic acids as potent antagonists of αvβ3/αvβ5 integrins

Abstract The synthesis and SAR of a new class of piperidine-based α v β 3 /α v β 5 integrin antagonists is described. Replacement of an amide bond in a prototype isonipecotamide by a C–C isostere, and adjustment of the spacer length between the carboxylic acid and basic moieties, led to low nanomolar antagonists of α v β 3 and/or α v β 5 integrins with excellent selectivity versus α IIb β 3 .