New ligands of the ghrelin receptor based on the 1,2,4-triazole scaffold by introduction of a second chiral center.

Bioorg Med Chem Lett

Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, ENSCM, Université de Montpellier, BP 14491, Faculté de Pharmacie, bât. E, 3(ème) étage, 15 avenue Charles Flahault, 34093 Montpellier Cedex 5, France. Electronic address:

Published: May 2016

Introducing a second chiral center on our previously described 1,2,4-triazole, allowed us to increase diversity and elongate the 'C-terminal part' of the molecule. Therefore, we were able to explore mimics of the substance P analogs described as inverse agonists. Some compounds presented affinities in the nanomolar range and potent biological activities, while one exhibited a partial inverse agonist behavior similar to a Substance P analog.

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http://dx.doi.org/10.1016/j.bmcl.2016.04.003DOI Listing

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