Discovery of l-(2,4-dichlorophenyl)4-ethyl-5-(5-(2-(4-(trifluoraethyl) phenyl) ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-lH-pyrazole-3- carboxamide as A Potential Peripheral Cannabinoid-1 Receptor Inverse Agonist

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Title:	Discovery of l-(2,4-dichlorophenyl)4-ethyl-5-(5-(2-(4-(trifluoraethyl) phenyl) ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-lH-pyrazole-3- carboxamide as A Potential Peripheral Cannabinoid-1 Receptor Inverse Agonist
Authors:	Chun-Ping Chang (張竣評) Ming-Shiu Hung Ting-Chieh Li Yinchiu Lin Yu-Sheng Chao Kak-Shan Shia (夏克山)
Date:	2011
Issue Date:	2011-06-23 14:57:17 (UTC+8)
Abstract:	A novel class of aryl alkynylthiophene compounds has been designed to target peripheral CB1R to eliminate/minimize CNS side effects as observed with 1, a typical brain CBlR-acting agent. The titled compound, l-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2 -yl)-N(piperidin-l-yl)-lH-pyrazole-3-carboxamide (8), is tentatively y recognhized as a peripheral inverse agonist based on its negative central effects in CB1R agonist-induced hypothermia and analgesia models, and low brain exposure (B/P = 1/33) measured at a time point of 2 hours following oral administration. The chronic study of 8 in DIO mice is currently underway. A full account of the in vivo studies, with particular emphasis on addressing issues of central drug accumulation and peripheral metabolic benefits, as well as further SAR studies on the series will be reported elsewhere in due course.
Relation:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
Appears in Collections:	[Pharmacy and Science] 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium

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