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Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists.

Abstract：

:5-Hydroxyalkyl-4-phenylpyridines have been identified as a novel class of glucagon antagonists with potential utility for the treatment of diabetes. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure-activity relationships led to the discovery of a potent antagonist, IC(50)=0.11 microM, more than 60-fold improvement over the lead structure.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ladouceur GH,Cook JH,Doherty EM,Schoen WR,MacDougall ML,Livingston JN

doi

10.1016/s0960-894x(01)00766-1

subject

Has Abstract

pub_date

2002-02-11 00:00:00

pages

461-4

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960894X01007661

journal_volume

12

pub_type

杂志文章

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