| Literature DB >> 14998340 |
Ji Yang1, Parviz Gharagozloo, Jiangchao Yao, Victor I Ilyin, Richard B Carter, Phong Nguyen, Silvia Robledo, Richard M Woodward, Derk J Hogenkamp.
Abstract
A series of 3-(4-phenoxyphenyl)-1H-pyrazoles were synthesized and characterized as potent state-dependent sodium channel blockers. A limited SAR study was carried out to delineate the chemical requirements for potency. The results indicate that the distal phenyl group is critical for activity but will tolerate lipophilic (+pi) electronegative (+sigma) substituents at the ortho and/or para position. Substitution at the pyrazole nitrogen with a H-bond donor improves potency. Compound 18 showed robust activity in the rat Chung neuropathy paradigm.Entities:
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Year: 2004 PMID： 14998340 DOI： 10.1021/jm030498q
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446