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Antimicrobial and cytotoxic activities of isoniazid connected menthone derivatives and their investigation of clinical pathogens causing infectious disease
- Source :
- Journal of Infection and Public Health, Vol 14, Iss 4, Pp 533-542 (2021)
- Publication Year :
- 2021
- Publisher :
- Elsevier BV, 2021.
-
Abstract
- Background This work is development of new molecules of isoniazid derivatives as dealing with potential of antimicrobial activity against clinical pathogens causing infectious disease. Antimicrobial of novel Mannich base derivatives can be achieved via one-pot synthesis in green chemistry approach. This method offers efficient, mild reaction conditions and high yields. In this study, totally 12 compounds (1a–l) was prepared and screened for cytotoxic and antimicrobial activities. Materials and methods Newly synthesised compounds were conformed via FT- IR, 1H, and 13C NMR (Nuclear Magnetic Resonance), and mass spectra analysis. All compounds were checked antibacterial activity against gram-positive bacteria of Enterococcus faecalis, Staphylococcus aureus and gram-negative bacteria of Pseudomonas aeruginosa, Klebsiella pneumoniae and Escherichia coli. All compounds were checked against antifungal activity against Aspergillus fumigatus, Candida albicans, Cryptococcus neoformans, Aspergillus niger, and Microsporum audouinii. All compounds were screened for cytotoxic activity against the MCF-7 (Michigan Cancer Foundation-7) cancer cell line. Result The compound 1g was highly (MIC: 0.25 μg/mL) active against gram-negative bacterial of P. aeruginosa, whereas other compounds 1e and 1h were more active (MIC: 2 μg/mL) in K. pneumoniae and also 1g (MIC: 2 μg/mL) was more active in E. faecalis than standard ciprofloxacin. Antifungal screening, the compound 1b was highly active (MIC: 0.25 μg/mL) against C. albicance, 1g (MIC: 2 μg/mL) and 1h (MIC: 4 μg/mL) was significant of active against A. fumigatus, and the compound 1c (MIC: 4 μg/mL) was extremely active in M. audouinii than clotrimazole. Compound 1g (GI50 = 0.01 μM) exhibited high activity against the MCF-7 cell line, while 1b (GI50 = 0.02 μM) was equipotent active compared with standard doxorubicin. Conclusion A novel set of isoniazid derivatives (1a–l) and 1h were synthesized and screened for antimicrobial and cytotoxic activities. We found some highly active molecules, which are evidencing to be a potential treatment of bacterial and fungal infection candidates.
- Subjects :
- 0301 basic medicine
Klebsiella pneumoniae
030106 microbiology
Microbial Sensitivity Tests
Menthone
Mannich base
Antifungal
Gram-Positive Bacteria
Communicable Diseases
Enterococcus faecalis
lcsh:Infectious and parasitic diseases
Aspergillus fumigatus
Microbiology
Structure-Activity Relationship
03 medical and health sciences
Minimum inhibitory concentration
0302 clinical medicine
Anti-Infective Agents
Gram-Negative Bacteria
Isoniazid
medicine
Humans
Microsporum
lcsh:RC109-216
030212 general & internal medicine
Grindstone Chemistry
biology
Chemistry
lcsh:Public aspects of medicine
Fungi
Public Health, Environmental and Occupational Health
lcsh:RA1-1270
General Medicine
biology.organism_classification
Antimicrobial
Antibacterial
Ciprofloxacin
Menthol
Infectious Diseases
Antibacterial activity
medicine.drug
Subjects
Details
- ISSN :
- 18760341
- Volume :
- 14
- Database :
- OpenAIRE
- Journal :
- Journal of Infection and Public Health
- Accession number :
- edsair.doi.dedup.....d010d7bce8cbf7067641361ebf587b8d
- Full Text :
- https://doi.org/10.1016/j.jiph.2020.12.033