Synthesis and biological profiling of novel isocoumarin derivatives and related compounds
| Autor: | Simić Milena R., Erić Slavica, Borić Ivan, Lubelska Annamaria, Latacz Gniewomir, Kiec-Kononowicz Katarzyna, Vojnović Sandra, Nikodinović-Runić Jasmina, Savić Vladimir M. |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: | |
| Zdroj: | Journal of the Serbian Chemical Society, Vol 86, Iss 7-8, Pp 639-649 (2021) |
| Druh dokumentu: | article |
| ISSN: | 0352-5139 1820-7421 |
| DOI: | 10.2298/JSC201201025S |
| Popis: | In the continuation of our study of substituted isocoumarins a series of novel 3-azolyl isocoumarin and their thio derivatives, including some related lactone compounds was prepared and biologically profiled against C. albicans showing moderate activity with MIC values in range of 4–60 g mL-1, in general. The additional characterisation of selected compounds was carried out by exploring their activity on CYP3A4 and CYP2D6 enzymes, while experiments on mutagenicity were performed by AMES test. The representative isocoumarins 3b, 4a and 4b showed lower inhibitory activity on CYP enzymes, when compared to the reference inhibitors, ketoconazole and quinidine. Compound 4a showed a higher mutagenic potential than the other two compounds. Further characterization included cytotoxicity profiling against normal MRC5 cells. |
| Databáze: | Directory of Open Access Journals |
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