Polović, Saša; Ljoljić Bilić, Vanja; Budimir, Ana; Kontrec, Darko; Galić, Nives; Kosalec, Ivan
(2019)
Antimicrobial assesment of aroylhydrazone
derivatives in vitro.
Acta pharmaceutica, 69
(2).
pp. 277-285.
ISSN 1330-0075
Abstract
Aroylhydrazones 1-13 were screened for antimicrobial and antibiofilm activities. N- (2- hydroxy-phenylmethylidene)-3- pyridinecarbohydrazide (2), N-(5-chloro-2- hydroxyphenylmethylidene)-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, respectively. 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 respective 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 MIC values (IC90 range 0.18–0.1 µmol mL–1). Good activity regarding multi-resistant clinical strains was observed for compound 12 against MRSA strain (MIC 0.020–0.023 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 shown for compounds 2 (MBFIC 0.015–0.02 µmol mL–1 against MRSA) and 12 (MBFIC 0.0132– 0.0134 µmol mL–1 against EBSL + E. coli).
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