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Molecules 2018, 23(1), 45; https://doi.org/10.3390/molecules23010045

Synthesis and Evaluation of Biological Activities of Aziridine Derivatives of Urea and Thiourea

1
Department of Microbial Genetics, Faculty of Biology and Environmental Protection, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland
2
Department of Organic and Applied Chemistry, Faculty of Chemistry, University of Lodz, Tamka 12, 91-403 Lodz, Poland
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 12 December 2017 / Revised: 19 December 2017 / Accepted: 21 December 2017 / Published: 25 December 2017
(This article belongs to the Section Bioorganic Chemistry)
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Abstract

In the present paper, we report the synthesis and evaluation of in vitro antimicrobial activities of aziridine-thiourea derivatives. A series of aziridines in reaction with isocyanates and isothiocyanates to obtain urea and thiourea derivatives were used. The structures of all new products were confirmed based on spectroscopic data (1H-NMR, 13C-NMR, HR-MS). These compounds were screened for their in vitro antimicrobial activity against a panel of Gram-positive and Gram-negative strains of bacteria. Six of the tested compounds appeared to be promising agents against reference strains of Escherichia coli, Staphylococcus aureus and Staphylococcus epidermidis. Subsequently, compounds exhibiting promising antibacterial activity were tested against twelve clinical isolates of S. aureus from three different sources of infection. The most bactericidal compounds (MIC = 16–32 µg/mL) showed better antibacterial activity against MRSA than ampicillin and streptomycin. The in vitro cytotoxicity analysis on L929 murine fibroblast and HeLa human tumor cell line using the MTT assay allowed us to select the least toxic compounds for future investigation. View Full-Text
Keywords: aziridines; thiourea derivatives; antimicrobial activity; cytotoxicity aziridines; thiourea derivatives; antimicrobial activity; cytotoxicity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Kowalczyk, A.; Pieczonka, A.M.; Rachwalski, M.; Leśniak, S.; Stączek, P. Synthesis and Evaluation of Biological Activities of Aziridine Derivatives of Urea and Thiourea. Molecules 2018, 23, 45.

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