کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10593817 | 981813 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4-one derivatives as inhibitors of the phosphatase SerB653 in Porphyromonas gingivalis, implicated in periodontitis
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کلمات کلیدی
HTSIC50MICPMSFIL-8haloacid dehalogenaseDMSO - DMSOMAPK - MAPKInterleukin-8 - اینترلوکین -8Minimum inhibitory concentration - حداقل غلظت مهاریDimethyl sulfoxide - دیمتیل سولفواکسیدphenylmethylsulfonyl fluoride - فنیل متیل سولفونیل فلورایدCompetitive inhibitor - مهار کننده رقابتhalf-maximal inhibitory concentration - نیمه حداکثر غلظت مهاریmitogen-activated protein kinase - پروتئین کیناز فعال با mitogenPeriodontitis - پریودنتیت
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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 IC50 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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 5, 1 March 2012, Pages 2084-2088
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 5, 1 March 2012, Pages 2084-2088
نویسندگان
Suk-Kyeong Jung, Youngkyung Ko, Keum Ran Yu, Ju Hee Kim, Joo-Youn Lee, Chong Hak Chae, Suk Ji, Chang Hyen Kim, Hyeon Kyu Lee, Eun Bok Choi, Bo Yeon Kim, Raymond L. Erikson, Sang J. Chung, Seung Jun Kim,