Romanian Society of Pharmaceutical Sciences

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ANTIMICROBIAL ACTIVITY INVESTIGATION OF SOME THIOSEMICARBAZIDES AND THEIR CYCLIZATION PRODUCTS

GABRIELA BĂNCESCU1, ŞTEFANIA-FELICIA BĂRBUCEANU2*, FLORICA BĂRBUCEANU3, GABRIEL ŞARAMET4, ADRIAN BĂNCESCU5, MIRCEA HÎRJĂU4

1University of Medicine and Pharmacy “Carol Davila”, Faculty of Dental Medicine, Discipline of Microbiology, Bucharest, Romania
2University of Medicine and Pharmacy “Carol Davila”, Faculty of Pharmacy, Discipline of Organic Chemistry, Bucharest, Romania
3Institute for Diagnosis and Animal Health, Bucharest, Romania
4University of Medicine and Pharmacy “Carol Davila”, Pharmaceutical Techniques Discipline, Faculty of Pharmacy, Bucharest, Romania
5University of Medicine and Pharmacy “Carol Davila”, Faculty of Medicine, Discipline of Microbiology-Epidemiology, Bucharest, Romania

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The aim of the present study was the investigation of the potential antimicrobial activity of some thiosemicarbazides (C1 and C2) and their cyclization products from 1,2,4- triazole (C3 and C4) and 1,3,4-thiadiazole (C5 and C6) class. All these compounds contain in their molecule X-C6H4SO2C6H4- (X=H, Br) and 2-F-C6H4- radicals and their synthesis was recently reported. The compounds C1-C6 have been tested against 10 reference microbial strains and 30 clinical fungal isolates using the broth microdilution method, in order to determine their minimum inhibitory concentrations (MIC) and minimum bactericidal/fungicidal concentrations (MBC/MFC), respectively. The MIC values ranged between: 32-256 μg/mL for thiosemicarbazide C1 and triazole C3, 128->512 μg/mL for thiosemicarbazide C2 and triazole C4, and 256->512 μg/mL for thiadiazoles C5 and C6. In all cases, the MBC/MIC or MFC/MIC ratio was less or equal to 4. As thiosemicarbazide C1 and triazole C3 presented the best antibacterial and antifungal activity from all studied compounds, it was considered that further investigations for these two compounds must be performed against more microbial strains.