925239-38-9

Upstream product

• 1912-33-0 Indole-3-acetic acid methyl ester 
• 5241-64-5 Boc-D-Trp-OH 
• 20781-20-8 2,4-Dimethoxybenzylamine 
• 5448-47-5 1H-indol-3-acetohydrazide 
• 87-51-4 indole-3-acetic acid 
• 937248-03-8 C₃₅H₃₈N₆O₄ 
• 937247-19-3 (R)-tert-butyl 1-(2,4-dimethoxybenzylamino)-3-(1H-indol-3-yl)-1-thioxopropan-2-ylcarbamate 
• 956489-57-9 (R)-tert-butyl 1-(2,4-dimethoxybenzylamino)-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamate 

Relevant academic research and scientific papers

Novel triazole derivatives as ligands of G-protein coupled receptors

The present invention provides novel triazole derivatives according to formula (I) as ligands of G-protein coupled receptors (GPCR), which are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, which are mediated by GPCR. The present invention further provides GPCR antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular adipogenesis, adiposity, cachexia, diabetes, diabetes type I, diabetes type II, energy balance, energy homeostasis, food intake, hyperlipidemia, hyperphagia, obesity, short-, medium- and/or long-term regulation of energy balance, short-, medium- and/or long-term regulation (stimulation and/or inhibition) of food intake.

Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors

The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions i

Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1

A new series of growth hormone secretagogue (GHS) analogues based on the 1,2,4-triazole structure were synthesized and evaluated for their in vitro binding and their ability to stimulate intracellular calcium release to the cloned hGHS-1a ghrelin receptor expressed in LLC PK-1 cells. We have synthesized potent ligands of this receptor, some of them behaving as agonists, partial agonists, or antagonists. Some compounds among the most potent, i.e., agonist 29c (JMV2873), partial agonists including 21b (JMV2810), antagonists 19b (JMV2866) and 19c (JMV2844), were evaluated for their in vivo activity on food intake, after sc injection in rodents. Some compounds were found to stimulate food intake like hexarelin; some others were identified as potent hexarelin antagonists in this assay. Among the tested compounds, 21b was identified as an in vitro ghrelin receptor partial agonist, as well as a potent in vivo antagonist of hexarelin-stimulated food intake in rodents. Compound 21b was without effect on GH release from rat. However, in this series of compounds, it was not possible to find a clear correlation between in vitro and in vivo results.