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Title 

Identification of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4-one derivatives as inhibitors of the phosphatase SerB653 in Porphyromonas gingivalis, implicated in periodontitis

Authors 

S K JungY KoKeum Ran YuJu Hee KimJ Y LeeC H ChaeS JiC H KimH K LeeE B ChoiBo Yeon KimR L EriksonSang Jeon ChungSeung Jun Kim

Publisher 

Elsevier

Issue Date 

2012

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 5, pp. 2084-2088

Keywords 

Competitive inhibitorGram-negative anaerobeHaloacid dehalogenaseHTSMalachite green colorimetric methodPeriodontitis --------------------------------------------------------------------------------

Abstract 

The serine phosphatase SerB653 plays a crucial role in the infection of Porphyromonas gingivalis, which contributes to the pathogenesis of periodontitis, an inflammatory disease of teeth-supporting tissues. Because functional loss of SerB653 eliminates the virulence of P. gingivalis, SerB653 inhibitors are considered potential periodontitis therapeutic or preventive agents. To identify SerB653 inhibitors with potent anti-periodontitis activity, we conducted a high-throughput screen of a representative 6800-compound subset of a synthetic chemical library of the Korea Chemical Bank (KCB) for compounds with activity against SerB653. The primary screening yielded 150 hits, and subsequent confirmatory studies identified eight compounds, mainly within a single cluster of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4-one derivatives, that showed greater than 50% inhibition of SerB653 activity at a concentration of 50 μM. A second screening with a focused library identified 10 compounds with IC 50 values less than 10 μM. In antibacterial tests, three of these compounds showed a minimum inhibitory concentration against P. gingivalis growth of 5-50 nM.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2012.01.011

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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