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Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists.

Abstract：

:The synthesis and biological evaluation of new potent opioid receptor-like 1 antagonists are presented. A structure-activity relationship (SAR) study of arylpyrazole lead compound 1 obtained from library screening identified compound 31, (1S,3R)-N-{[1-(3-chloropyridin-2-yl)-5-(5-fluoro-6-methylpyridin-3-yl)-4-methyl-1H-pyrazol-3-yl]methyl}-3-fluorocyclopentanamine, which exhibits high intrinsic potency and selectivity against other opioid receptors and hERG potassium channel.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kobayashi K,Uchiyama M,Ito H,Takahashi H,Yoshizumi T,Sakoh H,Nagatomi Y,Asai M,Miyazoe H,Tsujita T,Hirayama M,Ozaki S,Tani T,Ishii Y,Ohta H,Okamoto O

doi

10.1016/j.bmcl.2009.04.116

subject

Has Abstract

pub_date

2009-07-01 00:00:00

pages

3627-31

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00625-8

journal_volume

19

pub_type

杂志文章

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