1020809-13-5Relevant 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.
Heteroaryl-Pyrazole Derivatives as Cannabinoid CB1 Receptor Antagonists
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Page/Page column 69, (2008/06/13)
A heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing the inventive heteroaryl-pyrasole compounds or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity
Suk, Ho Lee,Hee, Jeong Seo,Lee, Sung-Han,Myung, Eun Jung,Park, Ji-Hyun,Park, Hyun-Ju,Yoo, Jakyung,Yun, Hoseop,Na, Jooran,Suk, Youn Kang,Song, Kwang-Seop,Kim, Min-Ah,Chang, Chong-Hwan,Kim, Jeongmin,Lee, Jinhwa
experimental part, p. 7216 - 7233 (2009/11/30)
Since the CB1 cannabinoid receptor antagonist 1 (SR141716, rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In the present study, biarylpyrazole analo
