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

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. (C) 2016 Elsevier Ltd. All rights reserved.