[Effective synthesis of cyclic analogs of bradykinin].
Cyclo-epsilon-(L-lysine1, glycine6-bradykinin) (CLGB) and cyclo-epsilon-kallidin have been synthesised in solution. To prepare linear precursors, fragment condensation (3 + 3 or 4) + 3 was used. Peptide bond formation, including cyclization, was carried out mainly through intermediate pentafluorophenyl esters. After purification on silicagel, protected cyclopeptides were obtained with a 50 to 60% yield. The protecting groups were eliminated by treatment with hydrogen fluoride in the presence of anisole. CLGB and CK were purified by droplet countercurrent chromatography and by reversed-phase HPLC, respectively.
Mutule
I E
IE
Mutulis
F K
FK
Erglis
D P
DP
Iakstrinia
D A
DA
Sekatsis
I P
IP
D001920:Bradykinin / Q000031:analogs & derivatives / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D007609:Kallidin / Q000031:analogs & derivatives / Q000138:chemical synthesis; D010456:Peptides, Cyclic / Q000138:chemical synthesis*
D010456:Peptides, Cyclic; D007609:Kallidin; D001920:Bradykinin
Effektivnyĭ sintez tsiklicheskikh analogov bradikinina.