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Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.

Abstract：

:Structure-activity relationship studies for two series of 2-benzyloxy-5-(4-chlorophenyl)-6-(2,4-dichlorophenyl)pyridines having either a 3-cyano or 3-carboxamide moiety resulted in the preparation of the 2-(3,4-difluorobenzyloxy)-3-nitrile analog 10d and the 2-(3,4-difluorobenzyloxy)-3-(N-propylcarboxamide) analog 16c, (hCB1 IC(50)=1.3 and 1.7 nM, respectively) as potent and selective hCB1 inverse agonists. Their synthesis and biological activities are described herein.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Meurer LC,Finke PE,Mills SG,Walsh TF,Toupence RB,Debenham JS,Goulet MT,Wang J,Tong X,Fong TM,Lao J,Schaeffer MT,Chen J,Shen CP,Sloan Stribling D,Shearman LP,Strack AM,Van der Ploeg LH

doi

10.1016/j.bmcl.2004.11.031

subject

Has Abstract

pub_date

2005-02-01 00:00:00

pages

645-51

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01389-7

journal_volume

15

pub_type

杂志文章

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