New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations

Journal of Medicinal Chemistry
Aline MoulinJean Martinez

Abstract

Ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure were synthesized and evaluated for their in vitro binding and biological activity. In this study, we explored the replacement of the alpha-aminoisobutyryl moiety by aromatic or heteroaromatic groups. Compounds 5 and 34 acted as potent in vivo antagonists of hexarelin-stimulated food intake. These two compounds did not stimulate growth hormone secretion in rodents and did not antagonize growth hormone secretion induced by hexarelin.

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Citations

May 11, 2012·Proceedings of the National Academy of Sciences of the United States of America·Sophie MaryJean-Louis Banères
Jun 23, 2012·Proceedings of the National Academy of Sciences of the United States of America·Shingo UenoTakafumi Sakai
Feb 18, 2010·PloS One·Guillaume OsterstockPierre-François Méry
Apr 1, 2009·Future Medicinal Chemistry·Luca Costantino, Daniela Barlocco
Jan 22, 2015·Proceedings of the National Academy of Sciences of the United States of America·Marjorie DamianJean-Louis Banères
Nov 10, 2009·Frontiers in Neuroendocrinology·T R CastañedaM H Tschöp
Sep 30, 2009·Journal of Peptide Science : an Official Publication of the European Peptide Society·Constance CholletAnnette G Beck-Sickinger
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Apr 28, 2012·Expert Opinion on Therapeutic Patents·Luca Costantino
Jul 23, 2014·Expert Opinion on Therapeutic Patents·Luca Costantino, Daniela Barlocco
May 9, 2014·Frontiers in Neurology·Carmela GiordanoGiuseppe Biagini
Aug 20, 2016·European Journal of Medicinal Chemistry·Jinqiang HouLeonard G Luyt
Jul 19, 2014·Journal of Medicinal Chemistry·Kimberly O CameronA Katrina Loomis
Dec 2, 2014·Bioorganic & Medicinal Chemistry Letters·Anne-Laure BlayoJean-Alain Fehrentz
Sep 13, 2015·The Journal of Biological Chemistry·Céline M'KadmiJacky Marie
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Jun 12, 2021·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Diana ZindelLaurent Prézeau

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