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2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists.

Abstract：

:Ghrelin, a gut-derived orexigenic hormone, is an endogenous ligand of the growth hormone secretagogue receptor (GHS-R). Centrally administered ghrelin has been shown to cause hunger and increase food intake in rodents. Inhibition of ghrelin actions with ghrelin antibody, peptidyl GHS-R antagonists, and antisense oligonucleosides resulted in weight loss and food intake decrease in rodents. Here we report the effects of GHS-R antagonists, some of which were potent, selective, and orally bioavailable. A structure-activity relationship study led to the discovery of 8a, which was effective in decreasing food intake and body weight in several acute rat studies.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Serby MD,Zhao H,Szczepankiewicz BG,Kosogof C,Xin Z,Liu B,Liu M,Nelson LT,Kaszubska W,Falls HD,Schaefer V,Bush EN,Shapiro R,Droz BA,Knourek-Segel VE,Fey TA,Brune ME,Beno DW,Turner TM,Collins CA,Jacobson PB,Sham H

doi

10.1021/jm0510934

subject

Has Abstract

pub_date

2006-04-20 00:00:00

pages

2568-78

issue

8

eissn

0022-2623

issn

1520-4804

journal_volume

49

pub_type

杂志文章

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