N-(4-Cyanotetrahydro-2 H-pyran-4-yl) and N-(1-Cyanocyclohexyl) Derivatives of 1, 5-Diarylpyrazole-3-carboxamides Showing High Affinity for 18 kDa Translocator …

SR Donohue, RF Dannals, C Halldin…

Index: Donohue, Sean R.; Dannals, Robert F.; Halldin, Christer; Pike, Victor W. Journal of Medicinal Chemistry, 2011 , vol. 54, # 8 p. 2961 - 2970

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Citation Number: 22

Abstract

In order to develop improved radioligands for imaging brain CB1 receptors with positron emission tomography (PET) based on rimonabant (5-(4-chlorophenyl)-1-(2, 4- dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1 H-pyrazole-3-carboxamide, 1), we synthesized compounds 9a− s in which the N-piperidinyl ring was replaced with a 4-(4-cyanotetrahydro- 2 H-pyranyl) or 1-cyanocyclohexyl ring. Such changes were expected to be almost ...