Literature DB >> 16359866

Partial structures of ketoconazole as modulators of the large conductance calcium-activated potassium channel (BK(Ca)).

Eoin C Power1, C Robin Ganellin, David C H Benton.   

Abstract

A series of partial structures of ketoconazole has been synthesized and tested for activity on the large conductance calcium-activated potassium channel (BK) in bovine smooth muscle cells. This has provided openers and blockers of the channel. The results suggest that the phenyl and phenoxy moieties are important for interaction with BK, whereas the imidazole group is unimportant. The properties of the phenoxy moiety seem to determine whether the compounds act to open or block the channel.

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Year:  2005        PMID: 16359866     DOI: 10.1016/j.bmcl.2005.11.001

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  In vivo and in vitro characterization of a first-in-class novel azole analog that targets pregnane X receptor activation.

Authors:  Madhukumar Venkatesh; Hongwei Wang; Julie Cayer; Melissa Leroux; Dany Salvail; Bhaskar Das; Jay E Wrobel; Sridhar Mani
Journal:  Mol Pharmacol       Date:  2011-04-04       Impact factor: 4.436

  1 in total

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