Current Enzyme Inhibition

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

DOI: 10.2174/1573408011666150408223245

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

Page: [46 - 57] Pages: 12

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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.

Graphical Abstract