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Synthesis and pharmacological characterization of functionalized 2-pyridones structurally related to the cardiotonic agent milrinone.

Abstract：

:A new class of cardiotonic agents characterized by a 2-pyridone structure was synthesized. Appropriate sym-2-dimethylaminomethylene-1,3-diones reacted with methylcyanoacetate to afford the desired compounds. These derivatives were evaluated for their ability in inducing cardiotonic response on guinea pig isolated myocardial preparations. Compound 8b increased atrial contractility to an extent which is significantly higher than that of milrinone, the parent drug used as a reference compound. The pharmacological characterization and the docking studies performed on 8b highlighted its selective mechanism of action via type 3 PDE (PDE3) inhibition.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Fossa P,Menozzi G,Dorigo P,Floreani M,Mosti L

doi

10.1016/s0968-0896(03)00528-5

subject

Has Abstract

pub_date

2003-11-03 00:00:00

pages

4749-59

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968089603005285

journal_volume

11

pub_type

杂志文章

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