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.
Andronati
Sergei A
SA
A.V. Bogatsky PhysicoChemical Institute of the National Academy of Sciences of Ukraine 86 Lustdorfskaya Doroga, 65080, Odessa, Ukraine. peptides@paco.net
Krysko
Andrei A
AA
Kabanov
Vladimir M
VM
Kabanova
Tatyana A
TA
Karaseva
Tamara L
TL
Chugunov
Boris M
BM
Meshkova
Svetlana B
SB
Topilova
Zoya M
ZM
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