New trisubstituted 1,2,4-triazoles as ghrelin receptor antagonists. - Archive ouverte HAL Access content directly
Journal Articles Bioorganic and Medicinal Chemistry Letters Year : 2015

New trisubstituted 1,2,4-triazoles as ghrelin receptor antagonists.

Abstract

Ghrelin receptor ligands based on a trisubstituted 1,2,4-triazole scaffold were recently synthesized and evaluated for their in vitro affinity for the GHS-R1a receptor and their biological activity. In this study, replacement of the α-aminoisobutyryl (Aib) moiety (a common feature present in numerous growth hormone secretagogues described in the literature) by aromatic and heteroaromatic groups was explored. We found potent antagonists incorporating the picolinic moiety in place of the Aib moiety. In an attempt to increase affinity and activity of our lead compound 2, we explored the modulation of the pyridine ring. Herein we report the design and the structure–activity relationships study of these new ghrelin receptor ligands.
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hal-01090274 , version 1 (03-12-2014)

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Anne-Laure Blayo, Mathieu Maingot, Babette Aicher, Céline M'Kadmi, Peter Schmidt, et al.. New trisubstituted 1,2,4-triazoles as ghrelin receptor antagonists.. Bioorganic and Medicinal Chemistry Letters, 2015, 25 (1), pp.20-24. ⟨10.1016/j.bmcl.2014.11.031⟩. ⟨hal-01090274⟩
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