288104-76-7Relevant 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
scheme or table, 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.
Oxadiazole-diarylpyrazole 4-carboxamides as cannabinoid CB1 receptor ligands
Lee, Suk Ho,Seo, Hee Jeong,Kim, Min Ju,Kang, Suk Youn,Song, Kwang-Seop,Lee, Sung-Han,Jung, Myung Eun,Kim, Jeongmin,Lee, Jinhwa
scheme or table, p. 1899 - 1902 (2009/11/30)
Cannabinoid CB-1 receptors have been the focus of extensive studies since the first clinical results of rimonabant (SR141716) for the treatment of obesity and obesity-related metabolic disorders were reported in 2001. To further evaluate the properties of
Pyrazolecarboxylic acid derivatives, their preparation, pharmaceutical compositions containing them
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, (2008/06/13)
N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-
