Structure-activity relationship study of position 4 in the urotensin-II receptor ligand U-II(4-11) |
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Authors: | Marzola Erika Camarda Valeria Batuwangala Madura Lambert David G Calo' Girolamo Guerrini Remo Trapella Claudio Regoli Domenico Tomatis Roberto Salvadori Severo |
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Institution: | Department of Pharmaceutical Sciences and Biotechnology Center, Section of Pharmacology, University of Ferrara, 44100 Ferrara, Italy. |
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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. |
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