Synthesis and bioactivities of nitronyl nitroxide and RGD containing pseudopeptides

Article abstract of DOI:10.1016/j.bmcl.2003.08.041

1-(1′,3′-dioxyl-4′,4′,5′,5′- tetramethyldihydroimidazol-2′-yl)-phenyl-4-yloxylacetic acid (3), and 1-(1′,3′-dioxyl-4′,4′,5′,5′- tetramethyldihydroimidazol-2′-yl)-phenyl-4-yloxylacetyl-RGDS (13), -RGDV (14), -RGDF (15) were synthesized. The ESR measurement gave the same spectroscopy for 3 and 13-15. The NO scavenging tests in vitro, anti-platelet aggregation tests in vitro and the anti-thrombosis assay in vivo indicated that introducing 3 into the N-terminal of RGDS, RGDV and RGDF the corresponding bioactivities for both of 3 and RGD peptides can be remained completely. The present combinations provided a beneficial strategy for simultaneous scavenging NO and anti-thrombosis, and for the use of spin label of RGD peptides in the conformational researches.