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Synthesis and in vitro antibacterial activity of new steroidal thiosemicarbazone derivatives

  作者 Khan, SA; Kumar, P; Joshi, R; Iqbal, PF; Saleem, K  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2008年43-9;  页码  2029-2034  
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[摘要]

We investigated the antibacterial activity of some new steroidal thiosemicarbazone derivatives, prepared from the reaction of cholest-5-en-7-one with thiosemicarbazides, in ethanol in the presence of a few drops of HCl at 80 degrees C in high yield. All the compounds have been characterized by means of elemental analyses, IR, H-1 NMR and mass spectroscopic data, to find an effective antibacterial agent. The antibacterial activity was first tested in vitro by the disk diffusion assay against two Gram-positive and two Gram-negative bacteria, and then the minimum inhibitory concentration (MIC) of compounds was determined. The results showed that the steroidal thiosemicarbazones derivatives inhibit growth of both types of the bacteria (Gram-positive and Gram-negative). The acetoxy and chloro derivatives of cyclopentyl and cyclohexyl amine thiosemicarbazones were found to have more antibacterial activity than the other derivatives. (C) 2008 Published by Elsevier Masson SAS.

 
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