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| Design, synthesis and biological evaluation of sulfenimine cephalosporin sulfoxides as β-lactamase inhibitors |
| Kai Zhanga, Huai-Wei Dinga, Hao Jua, Qi Huanga, Li-Juan Zhanga, Hong-Rui Songa, De-Cai Fub |
a Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China;
b College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018, China |
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Abstract A series of sulfenimine cephalosporin sulfoxide derivatives (7a-v) were designed, synthesized and evaluated for their inhibitory activity against TEM-1 and cephalosporinase in cell-free systems. Some of the tested compounds showed enhanced inhibitory activity against class C β-lactamase cephalosporinase compared with the tazobactam. The most promising compounds 7c and 7n (IC50 = 7.6 and 8.6 μmol/L, respectively) were further investigated in combination with cefradine against a variety of clinical isolated β-lactamase-producing bacterial strains.
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Received: 10 December 2014
Published: 18 April 2015
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Corresponding Authors:
Hong-Rui Song, De-Cai Fu
E-mail: hongruisong@163.com;dc6310@sina.com
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