Synthesis and antiaggregatory activity of RGD-peptidomimetics based on 4-oxo-4-(piperazine-1-yl)butyric acid as Arg-mimetic.
A scheme of synthesis of previously obtained RGDF-peptidomimetic-4-oxo-4-(piperazine-1-yl)butyrylglycyl-D,L-beta-phenyl-beta-alanine (I), was simplified. The novel RGDF-peptidomimetic -4-oxo-4-piperazine-1-yl)butyryl-glycyl-L-aspartyl-L-phenylalanine (II) was synthesized with the use of 4-oxo-4-(piperazine-1-yl)butyric acid as arginyl mimetic. The obtained pseudopeptides were able to inhibit both platelet aggregation in human blood and binding of fibrinogen to its receptor.
A.V. Bogatsky PhysicoChemical Institute of the National Academy of Sciences of Ukraine 86 Lustdorfskaya Doroga, 65080, Odessa, Ukraine. peptides@paco.net
Sergei A
SA
Andronati
Andrei A
AA
Krysko
Vladimir M
VM
Kabanov
Tatyana A
TA
Kabanova
Tamara L
TL
Karaseva
Boris M
BM
Chugunov
Svetlana B
SB
Meshkova
Zoya M
ZM
Topilova
D001792:Blood Platelets / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D005340:Fibrinogen / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011485:Protein Binding
C484802:4-oxo-4-(piperazine-1-yl)butyryl-glycyl-L-aspartyl-L-phenylalanine; D009842:Oligopeptides; D010879:Piperazines; D010975:Platelet Aggregation Inhibitors; C047981:arginyl-glycyl-aspartic acid; D005340:Fibrinogen