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.
Hung
Ming-Shiu
MS
Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35, Keyan Road, Zhunan Town, Miaoli County 35053, Taiwan, ROC.
Chang
Chun-Ping
CP
Li
Ting-Chieh
TC
Yeh
Teng-Kuang
TK
Song
Jen-Shin
JS
Lin
Yinchiu
Y
Wu
Chien-Huang
CH
Kuo
Po-Chu
PC
Amancha
Prashanth K
PK
Wong
Ying-Chieh
YC
Hsiao
Wen-Chi
WC
Chao
Yu-Sheng
YS
Shia
Kak-Shan
KS
D000818:Animals; D019440:Anti-Obesity Agents / Q000737:chemistry* / Q000494:pharmacology; D001812:Blood-Brain Barrier / Q000378:metabolism; D004195:Disease Models, Animal; D004353:Drug Evaluation, Preclinical; D054314:Drug Inverse Agonism; D006801:Humans; D007035:Hypothermia / Q000188:drug therapy; D008297:Male; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D043885:Receptor, Cannabinoid, CB2 / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
C554616:1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide; D019440:Anti-Obesity Agents; D011720:Pyrazoles; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; D013876:Thiophenes