Abstract

A series of tartronic acid analogs of a non-peptide RGD mimetic were prepared and evaluated both for antagonism of the vitronectin receptor and for affinity to hydroxyapatite, the main inorganic component of bone matrix. The hydroxy bis acid unit was found to be optimal for both receptor binding and hydroxyapatite affinity, while the N-terminus affected only receptor binding affinity.

Keywords: Arginine-Glycine-Aspartic Acid (rgd), vitronectin receptor, osteoporosis, tetracycline, aminotriazole, palladium-catalyzed coupling reactions, hydroxyapatite