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BIOEVALUATION OF THE ANTIMICROBIAL AND ANTI-PROLIFERATIVE POTENTIAL OF SOME DERIVATIVES OF 3,5-DINITRO-4-METHOXYAMINO-BENZOIC ACID

IRINA ZARAFU 1, BIANCA PĂTRAȘCU 1, LUMINIȚA MĂRUȚESCU 2, CORALIA BLEOTU 3, CARMEN LIMBAN 4, ARNAUD TATIBOUËT 5, MARIANA CARMEN CHIFIRIUC 2*, DIANA CAMELIA NUȚĂ 4, PETRE IONIȚĂ 1

1.University of Bucharest, Faculty of Chemistry, Organic Chemistry, Biochemistry and Catalysis Department, 90-92 Panduri Road, Bucharest, Romania
2 .University of Bucharest, Faculty of Biology and the Research Institute of the University of Bucharest, 91-95 Splaiul Independenței Street, Bucharest, Romania
3 .“Ștefan S. Nicolau” Institute of Virology, Cellular and Molecular Pathology Department, 285 Mihai Bravu Road, 030304, Bucharest, Romania
4 .“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Pharmaceutical Chemistry Department, 6 Traian Vuia Street, 020956, Bucharest, Romania
5 .University of Orleans, ICOA-UMR7311, CNRS, France

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The purpose of this study was to evaluate the anti-proliferative and antimicrobial activity of some derivatives of 3,5-dinitro-4-methoxyamino-benzoic acid previously obtained by coupling reactions of the above mentioned acid with benzylamine, n-butylamine, 4-amino-antipyrine, benzocaine, 3,4-dimethyl-5-amino-isoxazole, 3,4-dimethoxyphenyl-2-ethylamine and the corresponding methyl ester. The anti-tumoural activity was investigated on HCT8 cells, while the antimicrobial one was tested on bacterial and fungal cells, in planktonic and adherent growth state. The obtained compounds exhibited good antimicrobial activity, both against free-living, planktonic, as well as biofilm embedded Gram-positive bacterial and fungal cells, as well as anti-proliferative activity on the HCT8 cells. While PZ2, PZ6 and PZ7 compounds have shown a remarkable effect against planktonic microbial cells, PZ4 and PZ7 proved to be the most active anti-biofilm compounds. Considering their anti-tumoural potential, PZ1 and PZ7 proved to be the most cytotoxic against the HCT8 cells, inducing the HCT8 cells apoptosis and arrest in the G2/M phase of the cellular cycle.