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4-arylphthalazin-1(2H)-one derivatives as potent antagonists of the melanin concentrating hormone receptor 1 (MCH-R1).

Abstract：

:A novel series of 4-arylphthalazin-1(2H)-one linked to arylpiperidines were synthesized and evaluated as MCH-R1 antagonists. The results of an extensive SAR study probing the effects of substituents on the 4-arylphthalazin-1(2H)-one C-4 aryl group led to the identification of the 4-(3,4-difluorophenyl) derivative as a highly potent MCH-R1 inhibitor with an IC(50)=1nM. However, further investigations showed that this substance has unacceptable pharmacokinetic properties including a high clearance and volume of distribution.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

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

doi

10.1016/j.bmcl.2011.10.111

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

427-30

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01518-6

journal_volume

22

pub_type

杂志文章

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