In the present study we describe the synthesis and biological evaluation of 24 analogues of the urotensin II (U-II) fragment U-II(4-11) substituted in position 4 with coded and non-coded aromatic amino acids. All of the new analogues behaved as full U-II receptor (UT) agonists. Our results indicated that aromaticity is well tolerated, size, length and chirality of the side chain are not important, while substituents with a nitrogen atom are preferred. Thus acylation of U-II(5-11) with small groups bearing nitrogen atoms could be instrumental in future studies for the identification of novel potent UT receptor ligands.

Structure-activity relationship study of position 4 in the urotensin-II receptor ligand U-II(4-11)

MARZOLA, Erika;CAMARDA, Valeria;BATUWANGALA, Madura Suharshana;CALO', Girolamo;GUERRINI, Remo;TRAPELLA, Claudio;REGOLI, Domenico;TOMATIS, Roberto;SALVADORI, Severo
2008

Abstract

In the present study we describe the synthesis and biological evaluation of 24 analogues of the urotensin II (U-II) fragment U-II(4-11) substituted in position 4 with coded and non-coded aromatic amino acids. All of the new analogues behaved as full U-II receptor (UT) agonists. Our results indicated that aromaticity is well tolerated, size, length and chirality of the side chain are not important, while substituents with a nitrogen atom are preferred. Thus acylation of U-II(5-11) with small groups bearing nitrogen atoms could be instrumental in future studies for the identification of novel potent UT receptor ligands.
2008
Marzola, Erika; Camarda, Valeria; Batuwangala, Madura Suharshana; Lamberti, Dg; Calo', Girolamo; Guerrini, Remo; Trapella, Claudio; Regoli, Domenico; Tomatis, Roberto; Salvadori, Severo
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/471562
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