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Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity.

Abstract：

:Pyrido pyrimidinones are selective agonists of the human high affinity niacin receptor GPR109A (HM74A). They show no activity on the highly homologous low affinity receptor GPR109B (HM74). Starting from a high throughput screening hit the in vitro activity of the pyrido pyrimidinones was significantly improved providing lead compounds suitable for further optimization.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Peters JU,Kühne H,Dehmlow H,Grether U,Conte A,Hainzl D,Hertel C,Kratochwil NA,Otteneder M,Narquizian R,Panousis CG,Ricklin F,Röver S

doi

10.1016/j.bmcl.2010.07.108

subject

Has Abstract

pub_date

2010-09-15 00:00:00

pages

5426-30

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)01077-2

journal_volume

20

pub_type

杂志文章

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