Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists.

Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists. Research Abstract Details 

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Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists. Abstract Text:

Suk Youn Kang,Sung-Han Lee,Hee Jeong Seo,Myung Eun Jung,Kwangwoo Ahn,Jeongmin Kim,Jinhwa Lee,Suk Youn Kang,Sung-Han Lee,Hee Jeong Seo,Myung Eun Jung,Kwangwoo Ahn,Jeongmin Kim,Jinhwa Lee,

Cannabinoid CB1 receptors have been the focus of extensive studies since the first clinical results of rimonabant (SR141716) for the treatment of obesity and related metabolic disorders were reported in 2001. To further evaluate the properties of CB receptors, we have designed a new series of tetrazole-biarylpyrazoles. The various analogues were efficiently prepared and bio-assayed for binding to cannabinoid CB1 receptor. Six of the new compounds which displayed high in vitro CB1 binding affinities were assayed for binding to CB2 receptor. Noticeably, cyclopentyl-tetrazole (9a) demonstrated good binding affinity and selectivity for CB1 receptor (IC(50)=11.6nM and CB2/CB1=366).

Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists. Publishing Authors By Initials

SY Kang,SH Lee,HJ Seo,ME Jung,K Ahn,J Kim,J Lee,SY Kang,SH Lee,HJ Seo,ME Jung,K Ahn,J Kim,J Lee,

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Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 2385-9

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ISSN: 1464-3405

DAY: 29

MONTH: 02

YEAR: 2008

Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists.

AFFILIATION: Small Molecule Group, Central Research Institute, Green Cross Corporation, 341 Bojeong-Dong, Giheung-Gu, Yongin, Gyunggi-Do 446-799, Republic of Korea.

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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