Antimicrobial assesment of aroylhydrazone derivatives in vitro
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),...
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| Language: | English |
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Sciendo
2019-06-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.2478/acph-2019-0020 |
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| author | Polović Saša Bilić Vanja Ljoljić Budimir Ana Kontrec Darko Galić Nives Kosalec Ivan |
| author_facet | Polović Saša Bilić Vanja Ljoljić Budimir Ana Kontrec Darko Galić Nives Kosalec Ivan |
| author_sort | Polović Saša |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-42f7fc2d596e4867af0c0b1f2508e231 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2019-06-01 |
| publisher | Sciendo |
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| series | Acta Pharmaceutica |
| spelling | doaj-art-42f7fc2d596e4867af0c0b1f2508e2312025-02-02T15:22:11ZengSciendoActa Pharmaceutica1846-95582019-06-0169227728510.2478/acph-2019-0020acph-2019-0020Antimicrobial assesment of aroylhydrazone derivatives in vitroPolović Saša0Bilić Vanja Ljoljić1Budimir Ana2Kontrec Darko3Galić Nives4Kosalec Ivan5Agency for Medicinal Products and Medical Devices of Croatia Zagreb, CroatiaDepartment of Microbiology Faculty of Pharmacy and BiochemistryUniversity of Zagreb Zagreb, CroatiaDepartment of General and Inorganic Chemistry, Faculty of Pharmacy and Biochemistry, University of ZagrebZagreb, CroatiaDepartment of Organic Chemistry and Biochemistry, Ruđer Bošković Institute, PO Box 180, Zagreb, CroatiaDepartment of Chemistry Faculty of ScienceUniversity of Zagreb, Zagreb, CroatiaDepartment of Microbiology Faculty of Pharmacy and BiochemistryUniversity of Zagreb Zagreb, CroatiaAroylhydrazones 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.https://doi.org/10.2478/acph-2019-0020aroylhydrazonesantimicrobialantibiofilmmdr strains |
| spellingShingle | Polović Saša Bilić Vanja Ljoljić Budimir Ana Kontrec Darko Galić Nives Kosalec Ivan Antimicrobial assesment of aroylhydrazone derivatives in vitro Acta Pharmaceutica aroylhydrazones antimicrobial antibiofilm mdr strains |
| title | Antimicrobial assesment of aroylhydrazone derivatives in vitro |
| title_full | Antimicrobial assesment of aroylhydrazone derivatives in vitro |
| title_fullStr | Antimicrobial assesment of aroylhydrazone derivatives in vitro |
| title_full_unstemmed | Antimicrobial assesment of aroylhydrazone derivatives in vitro |
| title_short | Antimicrobial assesment of aroylhydrazone derivatives in vitro |
| title_sort | antimicrobial assesment of aroylhydrazone derivatives in vitro |
| topic | aroylhydrazones antimicrobial antibiofilm mdr strains |
| url | https://doi.org/10.2478/acph-2019-0020 |
| work_keys_str_mv | AT polovicsasa antimicrobialassesmentofaroylhydrazonederivativesinvitro AT bilicvanjaljoljic antimicrobialassesmentofaroylhydrazonederivativesinvitro AT budimirana antimicrobialassesmentofaroylhydrazonederivativesinvitro AT kontrecdarko antimicrobialassesmentofaroylhydrazonederivativesinvitro AT galicnives antimicrobialassesmentofaroylhydrazonederivativesinvitro AT kosalecivan antimicrobialassesmentofaroylhydrazonederivativesinvitro |