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SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.

Abstract：

:A high throughput screening campaign revealed compound 1 as a potent antagonist of the human CCK(1) receptor. Here, we report the syntheses and SAR studies of 1,5-diarylpyrazole analogs with various structural modifications of the alkane side chain of the molecule. The difference in affinity between the two enantiomers for the CCK(1) receptor and the flexible nature of the linker led to the design of constrained analogs with increased potency.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gomez L,Hack MD,McClure K,Sehon C,Huang L,Morton M,Li L,Barrett TD,Shankley N,Breitenbucher JG

doi

10.1016/j.bmcl.2007.09.093

subject

Has Abstract

pub_date

2007-12-01 00:00:00

pages

6493-8

issue

23

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)01147-X

journal_volume

17

pub_type

杂志文章

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