Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.

doi:10.1016/j.ejmech.2010.09.053

Paper

Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.

Published Dec 1, 2010 · R. Silvestri, A. Ligresti, G. La Regina

European journal of medicinal chemistry

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Abstract

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Animal Study

Study Snapshot

New N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides show greater hCB1 receptor affinity and can reduce food intake in rats when administered acutely.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.

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References

Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.

Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists show potential as effective oral modulators of CB1R.

Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand.

The 1,2,4-triazole-containing diarylpyrazolyl carboxamides show improved CB1 receptor binding affinity and excellent selectivity over CB2 receptors, offering potential for obesity treatment.

Novel thioamide derivatives as neutral CB1 receptor antagonists.

Novel thioamide derivatives show retained CB1 potency and improved solubility, with the neutral antagonist 2c significantly reducing body weight in cafeteria diet obese mice.

Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism.

Novel tacrine derivatives with combined acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism show promising potential for treating Alzheimer's disease.

Synthesis, cannabinoid receptor affinity, molecular modeling studies and in vivo pharmacological evaluation of new substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. 2. Effect of the 3-carboxamide substituent on the affinity and selectivity profile.

New substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides show potent affinity for the hCB1 receptor and comparable selectivity to reference compounds, with inhibition of food intake in rats.

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