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Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors |
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| Authors: | Eric J Gilbert Guowei Zhou Michael KC Wong Ling Tong Bandarpalle B Shankar Chunli Huang Joseph Kelly Brian J Lavey Stuart W McCombie Lei Chen Razia Rizvi Youhao Dong Youheng Shu Joseph A Kozlowski Neng-Yang Shih R William Hipkin Waldemar Gonsiorek Asra Malikzay Charles A Lunn Len Favreau Daniel J Lundell |
| Institution: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA;2. Department of Inflammation and Infectious Diseases, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA;3. Department of New Lead Discovery, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA;4. Department of Drug Metabolism, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA |
| Abstract: | The triaryl bis-sulfone 1 was modified by converting the aryl A-ring to a piperidine ring. The piperidine ring was further elaborated to a spirocyclopropyl piperidine moiety. The effect on CB2 binding potency, rat calcium channel affinity, and CYP 2C9 inhibition is described. |
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