Synthesis and bioactivities of nitronyl nitroxide and RGD containing pseudopeptides.
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.
College of Pharmaceutical Sciences, Peking University, Beijing 100083, P.R. China.
Junling
J
Liu
Ming
M
Zhao
Chao
C
Wang
Shiqi
S
Peng
D000595:Amino Acid Sequence; D009589:Nitrogen Oxides / Q000138:chemical synthesis* / Q000494:pharmacology*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry*; D013329:Structure-Activity Relationship
D009589:Nitrogen Oxides; D009842:Oligopeptides; C047981:arginyl-glycyl-aspartic acid; C039900:nitroxyl