RESUMO
The C-terminal (6-11)-hexapeptideamide Ala-Phe-Ile-Gly-Leu-Met-NH2 of eledoisin was synthesized by the solid phase method according to Merrifield. The alpha-amino group of alanine was acylated with heterocyclic or aromatic residues. These new compounds showed dose dependent hypotensive activities in the rabbit.
Assuntos
Anti-Hipertensivos/síntese química , Eledoisina/análogos & derivados , Animais , Pressão Sanguínea/efeitos dos fármacos , Eledoisina/síntese química , Eledoisina/farmacologia , Feminino , Frequência Cardíaca/efeitos dos fármacos , Masculino , Fragmentos de Peptídeos/síntese química , Fragmentos de Peptídeos/farmacologia , Coelhos , Fatores de TempoRESUMO
Dipeptides L-phenylalanyl-proline, D-phenylalanyl-proline, prolyl-valine, valyl-lysine, lysyl-leucine and leucyl-phenylalanine, derived from the sequence of gramicidin S, are substrates of the gramicidin S synthetase. When any of these dipeptides are used to replace the two corresponding amino acids in the reaction assay, cyclodecapeptide antibiotic synthesis occurs, and requires the whole multienzyme system. Active esters, like the thiophenyl and p-nitrophenyl esters of D-phenylalanyl-proline are unable to promote gramicidin S biosynthesis with the gramicidin S synthetase system or with the heavy enzyme alone.
