BAZI MICHAEL TIPI KATIM ÜRÜNLERININ SENTEZ ÇALISMASI VE ANTIMIKROBIYAL AKTIVITELER
| Autor: | Semra Utku, Gül Bayram, Mahmut Ülger, Erdoğan Berçin, Abdoul Nzeyimana, Gönül Aslan |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
2 amino 3 [(2 nitro 1 phenylpropyl)sulfanyl]propanoic acid
antibiotic resistance 2 amino 3 [[1 (4 chlorophenyl) 2 nitropropyl]sulfanyl]propanoic acid 2 amino 3 [[1 (4 methoxyphenyl) 2 nitropropyl]sulfanyl]propanoic acid 2 amino 3 [[1 [4 (dimethylamino)phenyl] 2 nitropropyl]sulfanyl]propanoic acid aromatic compound Enterococcus faecium 2 amino 3 [(2 nitro 1 phenylpropyl)thio]propanoic acid Pharmaceutical Science rifampicin proton nuclear magnetic resonance Michael type addition fluconazole resazurin Candida albicans antifungal agent Antifungal activity cysteine comparative study microtiter plate assay Chemistry 2 amino 3 [[1 (4 methylphenyl) 2 nitropropyl]sulfanyl]propanoic acid thin layer chromatography elemental analysis Fourier transform infrared spectroscopy broth dilution ethane Antimicrobial unclassified drug methyl- -nitrostyrene antiinfective agent retention time beta methyl beta nitrostyrene derivative Bacillus subtilis 2 amino 3 [[1 (4 nitrophenyl) 2 nitropropyl]sulfanyl]propanoic acid isoniazid in vitro study resazurin assay ?-methyl-?-nitrostyrene diastereoisomer drug design 2 amino 3 [[1 (4 hydroxy 3 methoxyphenyl) 2 nitropropyl]sulfanyl]propanoic acid minimum inhibitory concentration beta methyl beta nitrostyrene electrospray mass spectrometry benzaldehyde derivative Article Michael addition aldol reaction controlled study liquid chromatography-mass spectrometry Pharmacology antimicrobial activity nonhuman pharmacophore styrene derivative fungal strain Mycobacterium tuberculosis bacterial strain Combinatorial chemistry turbidity nitroethane drug structure Antimycobacterial activity chemical structure ampicillin drug synthesis tuberculostatic agent Antibacterial activity |
| Popis: | Objective: Multidrug-resistant pathogenic bacteria, fungi, and Mycobacterium tuberculosis infections continue to be increasingly widespread worldwide. In organic chemistry, the tiya-Michael type addition is also significant reaction in the synthesis of bioactive compounds. In this study, the aim is to synthesize the series of new Michael type addition products 2-amino-3-[(2-nitro-1-phenylpropyl)thio]propanoic acid (IIa-IIg) and to investigate their in vitro, antibacterial, antifungal and antitubercular activity. Material and Method: IIa-IIg derivatives were performed combining ?-methyl-?-nitrostyrenes (Ia-Ig) with L-cysteine using Michael addition reaction and characterized by 1HNMR, FTIR, ESI-LC/MS and elemental analysis. Microdilution method and resazurin microtiter assay were used to determine antimicrobial activities. Result and Discussion: Comparing the activities of the synthesized compounds, IIa, IId and IIe were found to have significant activity, with a MIC value of 1.95 ?g/ml, against Mycobacterium tuberculosis H37Rv strain. All synthesized novel compounds displayed moderate activity against tested bacterial and fungi strains. Among the synthesized compounds, IIb exhibited the best antibacterial and antifungal activity, with MIC values of 31.25, 31.25 and 15.6 ?g/ml, against B. subtilis, E. faecium and C. albicans, respectively. It was clear that some of the synthesized compounds exhibited antimycobacterial activity which could be a very good candidate for clinical uses. © 2022 University of Ankara. All rights reserved. This work was supported by the Mersin University Scientific Research Funds (Grant number |
| Databáze: | OpenAIRE |
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