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Discovery of a novel class of isoxazoline voltage gated sodium channel blockers |
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| Authors: | Pengcheng P. Shao Feng Ye Ann E. Weber Xiaohua Li Kathryn A. Lyons William H. Parsons Maria L. Garcia Birgit T. Priest McHardy M. Smith John P. Felix Brande S. Williams Gregory J. Kaczorowski Erin McGowan Catherine Abbadie William J. Martin Daniel R. McMasters Ying-Duo Gao |
| Affiliation: | aDepartment of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA;bDepartment of Ion Channels, Merck Research Laboratories, Rahway, NJ 07065, USA;cDepartment of Pharmacology, Merck Research Laboratories, Rahway, NJ 07065, USA;dDepartment of Molecular Modeling, Merck Research Laboratories, Rahway, NJ 07065, USA |
| Abstract: | Analogs of the previously reported voltage gated sodium channel blocker CDA54 were prepared in which one of the amide functions was replaced with aromatic and non-aromatic heterocycles. Replacement of the amide with an aromatic heterocycle resulted in significant loss of sodium channel blocking activity, while non-aromatic heterocycle replacements were well tolerated. |
| Keywords: | Voltage gated sodium channel blocker Neuropathic pain Inflammatory pain Amide replacement Heterocycles Isoxazoline |
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