Синтез и свойства 4-(1,2,3,4-тетрагидроизохинолин-7-ил)амино-4-оксо-бутаноил-D-β-фенил-β-аланина — нового RGDF миметика

Abstract

The novel RGDF mimetic, 4-(1,2,3,4-tetrahydroisoquinoline-7-yl)amino-4-oxobutyryl-D-β-phenyl-β-alanine, has been synthesized. Resulting from the conformational search, three groups of conformers have been revealed. It might be assumed on the base of NOESY spectroscopy data that the “extended” conformers are most likely realized in a DMSO solution. It is established that the synthesized peptidomimetic demonstrates a high in vitro antiaggregative activity (IC50 = 7.9 nM) and a high affinity to fibrinogen receptors (IC50 = 0.3 nM).