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1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists

Hou, Duen-Ren ; Alam, Safiul ; Kuan, Ting-Chun ; Ramanathan, Mani ; Lin, Tsung-Pang ; Hung, Ming-Shiu

Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.1022-1025 [Periódico revisado por pares]

Amsterdam: Elsevier Ltd

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Título:
1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists
Autor: Hou, Duen-Ren ; Alam, Safiul ; Kuan, Ting-Chun ; Ramanathan, Mani ; Lin, Tsung-Pang ; Hung, Ming-Shiu
Assuntos: Amides - chemistry ; Benzene - chemistry ; Biological and medical sciences ; Cannabinoid ; Cannabinoids - chemistry ; Chemistry, Pharmaceutical - methods ; Drug Design ; General and cellular metabolism. Vitamins ; Humans ; Inhibitory Concentration 50 ; Kinetics ; Ligands ; Medical sciences ; Miscellaneous ; Models, Chemical ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Obesity ; Obesity - drug therapy ; Pharmacology. Drug treatments ; Protein Binding ; Receptor, Cannabinoid, CB1 - antagonists & inhibitors ; Receptor, Cannabinoid, CB1 - metabolism ; Receptor, Cannabinoid, CB2 - antagonists & inhibitors ; Receptor, Cannabinoid, CB2 - metabolism ; Triazole ; Triazoles - chemical synthesis ; Triazoles - chemistry
É parte de: Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.1022-1025
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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Descrição: Development of new 1,2,3-triazoles as effective and selective CB1 receptor antagonists (IC 50 = 11.6 ± 3.4 nM; CB2/CB1 > 1000) is reported. This letter reports the new entry of novel 1,2,3-triazole derivatives as CB1 receptor antagonists. The design, synthesis and biological evaluation of N1 and N2 substituted 1,2,3-trizoles are described. The N2 substituted, symmetrical 1,2,3-triazoles are more potent ligands than the unsymmetrical analogues. The in vitro activity of these triazoles is further improved by inserting a methylene group between the central core and the carbonyl side chain. The most potent antagonists prepared in this series (IC 50 < 20 nM) are the triazoles containing benzyl amides. These triazoles also show excellent selectivity between CB1 and CB2 receptors (IC 50 > 10 μM for CB2; CB2/CB1 > 1000).
Editor: Amsterdam: Elsevier Ltd
Idioma: Inglês

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1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists

Hou, Duen-Ren ; Alam, Safiul ; Kuan, Ting-Chun ; Ramanathan, Mani ; Lin, Tsung-Pang ; Hung, Ming-Shiu

Amsterdam: Elsevier Ltd

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