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(2016) Novel synthesis scheme and invitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes, Journal of Enzyme Inhibition and Medicinal Chemistry, 31:6, 900-907, DOI: 10.3109/14756366.2015 AbstractDrug resistance has become a major concern in the field of infection management, therefore searching for new antibacterial agents is getting more challenging. Our study presents an optimized and eco-friendly synthesis scheme for a panel of nitroalkenes bearing various functional groups in the aromatic moiety and bromine or cyano substituents in 1 position of nitrovinyl moiety. The presence of nitrolefine group outside the ring minimalizes genotoxic properties while conjugation of aryl group with nitrovinyl moiety increases stability of the compounds. Then our research focused on evaluation of biological properties of such obtained (E)-2-aryl-1-cyano-1-nitroethenes. As they exhibit strong bacteriostatic and bactericidal activities against reference bacteria and yeast species with no detectable cytotoxicity towards cultured human HepG2 and HaCaT cells, they could be promising candidates for the replacement of traditional nitrofurane-containing antibacterial drugs. Nevertheless, validation of the obtained data in an in vivo model and additional safety studies on mutagenicity are still required.

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In this research, we synthesized and evaluated for in vitro antimicrobial activity a new series of hydrazide-hydrazones obtained from 5-nitrofuran-2-carboxylic acid.New compounds were identified and characterized by spectral methods ( 1 H NMR and 13 C NMR). All tested hydrazide-hydrazones proved to be promising antimicrobial agents. Antimicrobial activity and antifungal activity of new derivatives of 5-nitrofuran-2-carboxylic acid were revealed in many cases to be higher than the activity of reference substances (nitrofurantoin, cefuroxime and ampicillin). Yield: 47%; M.p.: 126°C; 1 H NMR (DMSO-d 6 ) δ (ppm): 2.09 (s, 3H, CH 3 ), 2.57-2.61 (t, 2H, CH 2 , J = 6 Hz), 2.68-2.74 (q, 2H, CH 2 , J = 6 Hz), 7.50-7.51 (d, 1H, ArH, J = 3 Hz), 7.78-7.79 (d, 1H, ArH, J = 3 Hz), 7.79-7.83 (t, 1H, =CH, J = 9 Hz, J = 3 Hz), 11.95 (s, 1H, NH); 13 C NMR (DMSO-d 6 ) δ (ppm): 14.6 (SCH 3 ), 30.3 (CH 2 ), 33.6 (CH 2 ), 115.4, 123.6, 138.2, 150.1 (4C ar ), 154.8 (=CH), 156.2 (C = O); For 262 | POPIOŁEK Et al.