Title:Cysteine and Its Derivatives as New Delhi Metallo-beta-lactamase-1 Inhibitors
Volume: 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
Affiliation:
Keywords:
IC50, NDM-1, cysteine, captopril, derivatives, inhibition.
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.