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

[ Vol. 11 , Issue. 1 ]

Author(s):

Cui-Gai Bai, Yin-Tong Xu, Ning-Ning Li, Jing-Han Wang, Cheng Yang, Yue Chen and Hong-Gang Zhou   Pages 46 - 57 ( 12 )

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.

Affiliation:

College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, P.R. China.

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