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Synthesis, biological evaluation, and metabolic stability of acrylamide derivatives as novel CCR3 antagonists.

Abstract：

:Our laboratory has identified several acrylamide derivatives with potent CCR3 inhibitory activity. In the present study, we evaluated the in vitro metabolic stability (CL(int); mL/min/kg) of these compounds in human liver microsomes (HLMs), and assessed the relationship between their structures and CL(int) values. Among the compounds identified, N-{(3R)-1-[(6-fluoro-2-naphthyl)methyl]pyrrolidin-3-yl}-2-[1-(2-hydroxybenzoyl)piperidin-4-ylidene]acetamide (30j) was found to be a potent inhibitor (IC(50)=8.4nM) with a high metabolic stability against HLMs.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Sato I,Morihira K,Inami H,Kubota H,Morokata T,Suzuki K,Ohno K,Iura Y,Nitta A,Imaoka T,Takahashi T,Takeuchi M,Ohta M,Tsukamoto S

doi

10.1016/j.bmc.2009.06.066

subject

Has Abstract

pub_date

2009-08-15 00:00:00

pages

5989-6002

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00640-3

journal_volume

17

pub_type

杂志文章

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