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Synthesis and SAR study of pyrrolo[3,4-b]pyridin-7(6H)-one derivatives as melanin concentrating hormone receptor 1 (MCH-R1) antagonists.

Abstract：

:The discovery and optimization of novel pyrrolo[3,4-b]pyridin-7(6H)-one MCH-R1 antagonists are described. A systematic SAR study probing the effects of aryl-, benzyl- and arylthio-substituents at the 2-position of the pyrrolo[3,4-b]pyridin-7(6H)-ones led to identification of the 2-[(4-fluorophenyl)thio] derivative 7b as a highly potent MCH-R1 antagonist. This compound also has favorable pharmacokinetic properties along with a high metabolic stability and a minimal impact on CYP isoforms and hERG.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lim CJ,Kim JY,Lee BH,Oh KS,Yi KY

doi

10.1016/j.bmcl.2013.01.053

subject

Has Abstract

pub_date

2013-03-15 00:00:00

pages

1736-9

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00086-3

journal_volume

23

pub_type

杂志文章

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