Cysteine and Its Derivatives as New Delhi Metallo-beta-lactamase-1 Inhibitors

Author(s): Cui-Gai Bai, Yin-Tong Xu, Ning-Ning Li, Jing-Han Wang, Cheng Yang, Yue Chen, Hong-Gang Zhou.

Journal Name: Current Enzyme Inhibition

Volume 11 , Issue 1 , 2015

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Abstract:

Nearly all antibiotics are ineffective to the antibiotic-resistant bacteria New Delhi metallo-beta -lactamase-1(NDM-1), one of the most important reasons is that antibiotics can be hydrolyzed by NDM-1 in these bacteria. Up to date, Many compounds, including captopril, are found to possess NDM-1 inhibition activity. Herein we report that some cysteine derivatives or homocysteine derivatives can inhibit the NDM-1 protein, and the lead compound 9 has the inhibition of the NDM-1 protein with IC50 of 1 µM, which is about 8 times potency of captopril.

Keywords: IC50, NDM-1, cysteine, captopril, derivatives, inhibition.

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Article Details

VOLUME: 11
ISSUE: 1
Year: 2015
Page: [46 - 57]
Pages: 12
DOI: 10.2174/1573408011666150408223245

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