Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity.

Abstract:

:A structure-activity relationship (SAR) study on the benzimidazole series of opioid receptor-like 1 (ORL1) antagonists related to 1 is described. Optimization of 1 by introduction of a hydrophilic substituent into the thioether part resulted in identification of potent ORL1 antagonists with high selectivity over binding affinity for hERG and other opioid receptors.

journal_name

Bioorg Med Chem Lett

authors

Kobayashi K,Kato T,Yamamoto I,Shimizu A,Mizutani S,Asai M,Kawamoto H,Ito S,Yoshizumi T,Hirayama M,Ozaki S,Ohta H,Okamoto O

doi

10.1016/j.bmcl.2009.04.022

subject

Has Abstract

pub_date

2009-06-01 00:00:00

pages

3100-3

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00488-0

journal_volume

19

pub_type

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