Design, synthesis and biological evaluation of 4-benzoyl-1-dichlorobenzoylthiosemicarbazides as potent Gram-positive antibacterial agents. (3rd May 2016)

• Record Type: Journal Article
• Authors: Paneth, Agata; Plech, Tomasz; Kaproń, Barbara; Hagel, Dominika; Kosikowska, Urszula; Kuśmierz, Edyta; Dzitko, Katarzyna; Paneth, Piotr
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 31:Number 3(2016:Jun.)
• Page Start: 434
• Page End: 440
• Publication Date: 2016-05-03
• Subjects: Antibacterial activity -- anti-biofilm activity -- MDR–MRSA -- MRSA -- MSSA -- thiosemicarbazide derivatives -- toxicity; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2015.1036050
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: Twelve 4-benzoyl-1-dichlorobenzoylthiosemicarbazides have been tested as potential antibacterials. All the compounds had MICs between 0.49 and 15.63 µg/ml toward Micrococcus luteus, Bacillus cereus, Bacillus subtilis and Staphylococcus epidermidis indicating, in most cases, equipotent or even more effective action than cefuroxime. In order to clarify if the observed antibacterial effects are universal, further research were undertaken to test inhibitory potency of two most potent compounds3 and11 on clinical isolates of Staphylococcus aureus . Compound11 inhibited the growth of methicillin-sensitive S. aureus (MSSA) at MICs of 1.95–7.81 µg/ml, methicillin-resistant S. aureus (MRSA) at MICs of 0.49–1.95 µg/ml and MDR–MRSA at MIC of 0.98 and 3.90 µg/ml, respectively. Finally, inhibitory efficacy of3 and11 on planktonic cells and biofilms formation in clinical isolates of S. aureus and Haemophilus parainfluenzae was tested. The majority of cells in biofilm populations of MSSA and MRSA were eradicated at low level of3, with MBICs in the range of 7.82–15.63 µg/ml.