Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.

Abstract:

:Structural features of the substituted 4-piperidinyl urea analogs 1, responsible for the H3 antagonist activity, have been identified. Structure-activity relationship of the H3 receptor affinity, hERG ion channel inhibitory activity and their separation is described. Preliminary pharmacokinetic evaluation of the compounds of the series is addressed.

journal_name

Bioorg Med Chem Lett

authors

Berlin M,Lee YJ,Boyce CW,Wang Y,Aslanian R,McCormick KD,Sorota S,Williams SM,West RE Jr,Korfmacher W

doi

10.1016/j.bmcl.2010.01.121

subject

Has Abstract

pub_date

2010-04-01 00:00:00

pages

2359-64

issue

7

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00133-2

journal_volume

20

pub_type

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