Abstract
Series of thirteen 1-[(2-chlorophenyl)carbamoyl]naphthalen-2-yl carbamates and thirteen 1-[(2-nitrophenyl)carbamoyl]naphthalen-2-yl carbamates with alkyl/cycloalkyl/arylalkyl chains were prepared and characterized. Primary in vitro screening of the synthesized compounds was performed against Staphylococcus aureus, two methicillin-resistant S. aureus strains, Mycobacterium marinum, and M. kansasii. 1-[(2-Chlorophenyl)carbamoyl]naphthalen-2-yl ethylcarbamate and 1-[(2-nitrophenyl)carbamoyl]naphthalen-2-yl ethylcarbamate showed antistaphylococcal (MICs = 42 µM against MRSA) and antimycobacterial (MICs = 21 µM) activity against the tested strains comparable with or higher than that of the standards ampicillin and isoniazid. In the case of bulkier carbamate tails (R > propyl/isopropyl), the activity was similar (MICs ca. 70 µM). Screening of the cytotoxicity of both of the most effective compounds was performed using THP-1 cells, and no significant lethal effect was observed (LD50 >30 µM). The structure-activity relationships are discussed.
Highlights
Infectious diseases represent an increasing worldwide threat
All compounds were tested for their in vitro antimicrobial activity against S. aureus, two methicillin-resistant
The biological activity of the compounds is dependent on the alkyl substitution of carbamate nitrogen
Summary
Infectious diseases represent an increasing worldwide threat. The number of untreatable diseases decreased after the 1950s due to the introduction of new antimicrobial agents. The increase in the number of new infections is caused by general immunosuppression, a significant increase in the number of diabetic or HIV-positive patients, and the development of resistance to commonly used drugs. The resistance of common pathogens to first-choice drugs increased by up to 100% during the last few decades. The resistance of some strains to second- or third-choice drugs can be found.
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