1217348-10-1Relevant academic research and scientific papers
Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand
Seo, Hee Jeong,Kim, Min Ju,Lee, Suk Ho,Lee, Sung-Han,Jung, Myung Eun,Kim, Mi-Soon,Ahn, Kwangwoo,Kim, Jeongmin,Lee, Jinhwa
experimental part, p. 1149 - 1162 (2010/04/24)
Numerous research groups have been engaged in searching for novel CB1 receptor antagonists, since SR141716A (rimonabant), a CB1 receptor antagonist, proved to be efficacious in human for the treatment of obesity. In the present study, a series of 1,2,4-triazole-containing diarylpyrazolyl carboxamides based on the 1,5-diarylpyrazole template of rimonabant, was synthesized and tested for CB1 receptor binding affinity. The structure-activity relationship studies demonstrated that incorporation of 1,2,4-triazole ring onto the pyrazole scaffold via a methylene linker led to a significant improvement for CB1 receptor binding affinity. Importantly, these analogues also exhibited excellent selectivity for CB1 receptor over CB2 receptor.
