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| Antibacterial activity of piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline |
| SHAN Keming1, LI Tianyi2, PU Ji2,3 |
| 1. Planning and Research Institute, China North Industries Group Corporation, Beijing 100053, China; 2. State Key Laboratory for Infectious Disease Prevention and Control, National Institute for Communicable Disease Control and Prevention, Chinese Center for Disease Control and Prevention, Beijing 102206, China; 3. Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases, Hangzhou 310003, China |
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Abstract Antibacterial activity of fifteen piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline was investigated in order to search for compounds with efficient antibacterial activity. First, the binding energies of substrate-enzyme were predicted by molecular docking calculation. Second, minimum inhibitory concentration (MIC) values of the tested compounds were measured against the multidrug-resistant Escherichia coli (E. coli) with a standard method. The results showed that some compounds had better antibacterial activity than the control, and MIC of compounds 7a, 7g and 7k was below 1 mg/mL. The results were further confirmed by high performance capillary electrophoresis (HPCE) screening method, and the half inhibitory concentration (IC50) of 7k was 4.97×10－2 mg/mL. In addition, structure-activity relationship analysis showed that the presence of an electron-withdrawing group at the C2-position of phenyl ring linked with piperazine moiety was favorable to the antibacterial activity. This study provided a new option for the development of antimicrobial agents.
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Received: 24 February 2016
Published: 25 June 2016
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Corresponding Authors:
PU Ji
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2016, Vol. 11 
