<abstract xmlns="http://www.w3.org/1999/xhtml">Aroylhydrazones <bold>1–13</bold> were screened for antimicrobial and antibiofilm activities <italic>in vitro. N′</italic>-(2-hydroxy-phenylmethylidene)-3-pyridinecarbohydrazide (<bold>2</bold>), <italic>N′</italic>-(5-chloro-2-hydroxyphenyl-methylidene)-3-pyridinecarbohydrazide (<bold>10</bold>), <italic>N′</italic>-(3,5-chloro-2-hydroxyphenylmethylidene)-3-pyridinecarbohydrazide (<bold>11</bold>), and <italic>N′</italic>-(2-hydroxy-5-nitrophenylmethylidene)-3-pyridinecarbohydrazide (<bold>12</bold>) showed antibacterial activity against <italic>Escherichia coli</italic>, with <italic>MIC</italic> values (in µmol mL−1) of 0.18–0.23, 0.11–0.20, 0.16–0.17 and 0.35–0.37, resp. Compounds <bold>11</bold> and <bold>12</bold>, as well as <italic>N′</italic>-(2-hydroxy-3-methoxyphenylmethylidene)-3-pyridinecarbohydrazide (<bold>6</bold>) and <italic>N′</italic>-(2-hydroxy-5- methoxyphenylmethylidene)-3-pyridinecarbohydrazide (<bold>8</bold>) showed antibacterial activity against <italic>Staphylococcus aureus</italic>, with the lowest <italic>MIC</italic> values of 0.005–0.2, 0.05–0.12, 0.06–0.48 and 0.17–0.99 µmol mL−1. <italic>N′</italic>-(2-hydroxy-5-methoxyphenylmethylidene)-3-pyridinecarbohydrazide (<bold>7</bold>) showed antifungal activity against both fluconazole resistant and susceptible <italic>C. albicans</italic> strains with <italic>IC</italic>90 range of 0.18–0.1 µmol mL−1. Only compound <bold>11</bold> showed activity against <italic>C. albicans</italic> ATCC 10231 comparable to the activity of nystatin (the lowest <italic>MIC</italic> 4.0 ×10−2<italic>vs</italic>. 1.7 × 10−2 µmol mL−1). Good activity regarding multi-resistant clinical strains was observed for compound <bold>12</bold> against MRSA strain (<italic>MIC</italic> 0.02 µmol mL−1) and compounds <bold>2</bold>, <bold>6</bold> and <bold>12</bold> against ESBL+ <italic>E. coli</italic> MFBF 12794, with the lowest <italic>MIC</italic> for compound <bold>12</bold> (<italic>IC</italic>50 0.16 µmol mL−1). Anti-biofilm activity was found for compounds <bold>2</bold> (<italic>MBFIC</italic> 0.015–0.02 µmol mL−1 against MRSA) and <bold>12</bold> (<italic>MBFIC</italic> 0.013 µmol mL−1 against EBSL+ <italic>E. coli</italic>). In the case of compound <bold>2</bold> against MRSA biofilm formation, <italic>MBFIC</italic> values were comparable to those of gentamicin sulphate, whereas in the case of compound <bold>12</bold> and EBSL+ <italic>E. coli</italic> even more favourable activity compared to gentamicin was observed.</abstract>

Aroylhydrazones 1–13 were screened for antimicrobial and antibiofilm activities in vitro. N′-(2-hydroxy-phenylmethylidene)-3-pyridinecarbohydrazide (2), N′-(5-chloro-2-hydroxyphenyl-methylidene)-3-pyridinecarbohydrazide (10), N′-(3,5-chloro-2-hydroxyphenylmethylidene)-3-pyridinecarbohydrazide (11), and N′-(2-hydroxy-5-nitrophenylmethylidene)-3-pyridinecarbohydrazide (12) showed antibacterial activity against Escherichia coli, with MIC values (in µmol mL−1) of 0.18–0.23, 0.11–0.20, 0.16–0.17 and 0.35–0.37, resp. Compounds 11 and 12, as well as N′-(2-hydroxy-3-methoxyphenylmethylidene)-3-pyridinecarbohydrazide (6) and N′-(2-hydroxy-5- methoxyphenylmethylidene)-3-pyridinecarbohydrazide (8) showed antibacterial activity against Staphylococcus aureus, with the lowest MIC values of 0.005–0.2, 0.05–0.12, 0.06–0.48 and 0.17–0.99 µmol mL−1. N′-(2-hydroxy-5-methoxyphenylmethylidene)-3-pyridinecarbohydrazide (7) showed antifungal activity against both fluconazole resistant and susceptible C. albicans strains with IC90 range of 0.18–0.1 µmol mL−1. Only compound 11 showed activity against C. albicans ATCC 10231 comparable to the activity of nystatin (the lowest MIC 4.0 ×10−2vs. 1.7 × 10−2 µmol mL−1). Good activity regarding multi-resistant clinical strains was observed for compound 12 against MRSA strain (MIC 0.02 µmol mL−1) and compounds 2, 6 and 12 against ESBL+ E. coli MFBF 12794, with the lowest MIC for compound 12 (IC50 0.16 µmol mL−1). Anti-biofilm activity was found for compounds 2 (MBFIC 0.015–0.02 µmol mL−1 against MRSA) and 12 (MBFIC 0.013 µmol mL−1 against EBSL+ E. coli). In the case of compound 2 against MRSA biofilm formation, MBFIC values were comparable to those of gentamicin sulphate, whereas in the case of compound 12 and EBSL+ E. coli even more favourable activity compared to gentamicin was observed.

Antimicrobial assesment of aroylhydrazone derivatives <italic>in vitro</italic>

Department of Microbiology Faculty of Pharmacy and Biochemistry

Department of General and Inorganic Chemistry, Faculty of Pharmacy and Biochemistry

Department of Organic Chemistry and Biochemistry

Department of Chemistry Faculty of Science

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Antimicrobial assesment of aroylhydrazone derivatives 

Aroylhydrazones 1–13 were screened for antimicrobial and antibiofilm activities in vitro. N′-(2-hydroxy-phenylmethylidene)-3-pyridinecarbohydrazide (2),...

Antimicrobial assesment of aroylhydrazone derivatives in vitro

Publicado en línea: 28 mar 2019

Páginas: 277 - 285

Aceptado: 14 dic 2018

DOI: https://doi.org/10.2478/acph-2019-0020

Palabras clave
aroylhydrazones, antimicrobial, antibiofilm, MDR strains

© 2019 Saša Polović et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Antimicrobial assesment of aroylhydrazone derivatives in vitro

Publicado en línea: 28 mar 2019

Páginas: 277 - 285

Aceptado: 14 dic 2018

DOI: https://doi.org/10.2478/acph-2019-0020

Palabras clavearoylhydrazones, antimicrobial, antibiofilm, MDR strains

© 2019 Saša Polović et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Palabras clave
aroylhydrazones, antimicrobial, antibiofilm, MDR strains