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Background  Bacterial multidrug resistance (MDR) constitutes a major hurdle in the treatment of infectious diseases worldwide. The present study was designed to evaluate the antibacterial activities of synthetic  p -toluenesulfonyl-hydrazinothiazoles against multidrug resistant Gram-negative bacteria.    Methods  The broth microdilution method was used to determine the minimal inhibitory concentrations (MIC).    Results  The results demonstrated that the best activities were obtained with hydrazinoselenazoles.  p -Chloro-benzyliden-selenosemicarbazide, 4-methyl-2-[(4-chloro-benzyliden)-hydrazinyl]-1,3-selenazole,  p -chloro-benzoyl-selenosemicarbazide and 4-chloromethyl-2-[(4-chlorobenziliden)- N -acetyl-hydrazinyl]-1,3-selenazole were more active than the choramphenicol on  Klebsiella pneumoniae  KP63. Tested alone, the lowest MIC value of 16 mg/L was obtained with  p -methoxy-benzyliden-selenosemicarbazide against  Enterobacter aerogenes  ATCC13048,  K. pneumoniae  ATCC112296 and KP55. Tested in the presence of an efflux pump inhibitor, phenylalanine arginine  β -naphthylamide (PAβN), the activity of  p -chloro-benzyliden-selenosemicarbazide, 4-methyl-2-[(4-chloro-benzyliden)-hydrazinyl]-1,3-selenazole,  p -chloro-benzoyl-selenosemicarbazide and  p -methoxy-benzyliden-selenosemicarbazide significantly increased with MIC values below 10 mg/L obtained respectively on 43.8 %, 31.3 %, 62.5 % and 100 % of the 16 tested bacterial strains. The lowest MIC value of 0.5 mg/L in the presence of PAβN was recorded with  p -chloro-benzoyl-selenosemicarbazide against  Escherichia coli  ATCC8739 and KP55 as well as  p -methoxy-benzyliden-selenosemicarbazide against  E. aerogenes  KP55.  p -Chloro-benzyliden-selenosemicarbazide and  p -chloro-benzoyl-selenosemicarbazide contained the same pharmacophore as  p -methoxy-benzyliden-selenosemicarbazide.    Conclusion  This study indicates that  p -chloro-benzyliden-selenosemicarbazide,  p -chloro-benzoyl-selenosemicarbazide and  p -methoxy-benzyliden-selenosemicarbazide could be explored more to develop novel antimicrobial drugs to fight MDR bacterial infections.

bmc pharmacology and toxicology

In vitro antibacterial activities of p-toluenesulfonyl-hydrazinothiazoles and hydrazinoselenazoles against multi-drug resistant Gram-negative phenotypes