Synthesis and biological activity of the mono- and di-galactosyl-vespulakinin 1 analogues.
作者： M. GOBBO , L. BIONDI , F. FILIRA , B. SCOLARO , R. ROCCHI
DOI: 10.1111/J.1399-3011.1992.TB00104.X
关键词:
摘要: Syntheses are described of some mono- and di-glycosylated analogues vespulakinin 1. The solid phase procedure, based on the Fmoc chemistry, was used to prepare (Gal alpha)Thr3-vespulakinin 1, beta)Thr3-vespulakinin 1 analogue ((Gal alpha)Thr3, alpha)Thr4-vespulakinin beta-glycosylated derivative also prepared by continuous flow variant polyamide method. synthesized glycopeptides were purified characterized amino acid analysis, optical rotation, analytical HPLC, 1H- 13C-NMR FAB-MS. Preliminary pharmacological experiments showed that carbohydrate-free is less active than bradykinin (about 0.3 times a molar basis) when tested guinea pig rectum contraction, two monoglycosylated equiactive 0.9 activity). most derivative, analogue, about 2.5 as bradykinin.
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