Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist

ChemMedChem. 2010 Sep 3;5(9):1439-43. doi: 10.1002/cmdc.201000246.

Authors

Ming-Shiu Hung¹, Chun-Ping Chang, Ting-Chieh Li, Teng-Kuang Yeh, Jen-Shin Song, Yinchiu Lin, Chien-Huang Wu, Po-Chu Kuo, Prashanth K Amancha, Ying-Chieh Wong, Wen-Chi Hsiao, Yu-Sheng Chao, Kak-Shan Shia

Affiliation

¹ Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35, Keyan Road, Zhunan Town, Miaoli County 35053, Taiwan, ROC.

PMID: 20652930
DOI: 10.1002/cmdc.201000246

No abstract available

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Anti-Obesity Agents / chemistry*
Anti-Obesity Agents / pharmacology
Blood-Brain Barrier / metabolism
Disease Models, Animal
Drug Evaluation, Preclinical
Drug Inverse Agonism
Humans
Hypothermia / drug therapy
Male
Pyrazoles / chemical synthesis
Pyrazoles / chemistry*
Pyrazoles / pharmacokinetics
Rats
Rats, Sprague-Dawley
Receptor, Cannabinoid, CB1 / antagonists & inhibitors*
Receptor, Cannabinoid, CB1 / metabolism
Receptor, Cannabinoid, CB2 / antagonists & inhibitors
Receptor, Cannabinoid, CB2 / metabolism
Structure-Activity Relationship
Thiophenes / chemical synthesis
Thiophenes / chemistry*
Thiophenes / pharmacokinetics

Substances

1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide
Anti-Obesity Agents
Pyrazoles
Receptor, Cannabinoid, CB1
Receptor, Cannabinoid, CB2
Thiophenes