当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists.

Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists.

Abstract：

:A structure-activity relationship study was undertaken to address the lack of oral exposure of the H3 antagonist 1, which incorporated an arylketone. Among a number of sub-series, the 4H-pyrido[1,2-a]pyrimidin-4-one analog 21 showed an improved PK profile in rat and mouse and was active in an obesity model. The pyrimidin-4-one proved to be a novel and useful ketone bioisostere.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Xiao D,Palani A,Sofolarides M,Aslanian R,West RE Jr,Williams SM,Wu RL,Hwa J,Sondey C,Lachowicz J,Korfmacher WA

doi

10.1016/j.bmcl.2012.02.076

subject

Has Abstract

pub_date

2012-05-01 00:00:00

pages

3354-7

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00277-6

journal_volume

22

pub_type

杂志文章

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