Dihydroisoquinolone RGD mimics. Exploration of the aspartate isostere

Article abstract of DOI:10.1016/S0960-894X(97)10014-2

Disubstituted 3,4-dihydroisoquinolones that contain an ether-linked benzamidine at C₆ and a β-substituted aspartate mimic at C₂ offer enhanced affinity for GPIIb-IIIa relative to the non-substituted isoquinolone propionate. Alkyl substituents afforded a 10-fold increase in intrinsic activity while aryl substituents yielded a 40-fold improvement.