Synthesis of substituted 4( Z)-(methoxyimino)pentyl-1-piperidines as dual NK 1/NK 2 inhibitors

The NK 1 and NK 2 receptor activity of a series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4( Z)-(methoxyimino)pentyl-1-piperidines was evaluated. Compounds 11d, 11e, 11f, 12a, and 12k were found to be our most potent inhibitors. A series of 4( Z)-(methoxyimino)pentyl-1-pi...

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Published inBioorganic & medicinal chemistry letters Vol. 11; no. 4; pp. 491 - 494
Main Authors Ting, Pauline C, Lee, Joe F, Anthes, John C, Shih, Neng-Yang, Piwinski, John J
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 26.02.2001
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Summary:The NK 1 and NK 2 receptor activity of a series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4( Z)-(methoxyimino)pentyl-1-piperidines was evaluated. Compounds 11d, 11e, 11f, 12a, and 12k were found to be our most potent inhibitors. A series of 4( Z)-(methoxyimino)pentyl-1-piperidines was prepared, and their biological activity as dual NK 1/NK 2 receptor antagonists determined. Analogues containing a substituted piperidinylpiperidine moiety displayed nanomolar potency for both the NK 1 and NK 2 receptors.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00702-2