Cui-Gai Bai, Yin-Tong Xu, Ning-Ning Li, Jing-Han Wang, Cheng Yang, Yue Chen and Hong-Gang Zhou Pages 46 - 57 ( 12 )
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.
IC50, NDM-1, cysteine, captopril, derivatives, inhibition.
College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, P.R. China.