Citation: Kai Zhang, Huai-Wei Ding, Hao Ju, Qi Huang, Li-Juan Zhang, Hong-Rui Song, De-Cai Fu. Design, synthesis and biological evaluation of sulfenimine cephalosporin sulfoxides as β-lactamase inhibitors[J]. Chinese Chemical Letters, ;2015, 26(6): 801-803. doi: 10.1016/j.cclet.2015.04.025 shu

Design, synthesis and biological evaluation of sulfenimine cephalosporin sulfoxides as β-lactamase inhibitors

Kai Zhang ^a ,
Huai-Wei Ding ^a ,
Hao Ju ^a ,
Qi Huang ^a ,
Li-Juan Zhang ^a ,
Hong-Rui Song ^a,, ,
De-Cai Fu ^b,,

1.
a Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China;
2.
b College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018, China

Corresponding author: Hong-Rui Song, De-Cai Fu,
Received Date: 10 December 2014
Available Online: 24 March 2015

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.
- β-Lactamase inhibitor,
- Sulfenimine,
- Synthesis
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