Study of the Activity and Toxicity of New Antibacterial Agents Based on Triindolylmethane Derivatives in vivo
Biological properties of new synthetic triindolylmethylium antibiotics of the triindolylmethane group, including compounds containing a maleimide fragment in the structure, are studied. Their high antibacterial activity in vitro, mainly against gram-positive bacteria, but also against strains with m...
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| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | Russian |
| Published: |
LLC "Publishing House OKI"
2020-05-01
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| Series: | Антибиотики и Химиотерапия |
| Subjects: | |
| Online Access: | https://www.antibiotics-chemotherapy.ru/jour/article/view/104 |
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| Summary: | Biological properties of new synthetic triindolylmethylium antibiotics of the triindolylmethane group, including compounds containing a maleimide fragment in the structure, are studied. Their high antibacterial activity in vitro, mainly against gram-positive bacteria, but also against strains with multiple drug resistance, was shown. The compounds, that showed the least in vitro toxicity on human donor fibroblasts PF-hTERT, were subjected to further testing in animals (mice). The LD50 and LD10 values identified were 24.2 and 16.9 mg/kg, respectively, for LCTA-2701 compound and 41.8 and 34.1 mg/kg for LCTA-2841 compound. In vivo testing of chimeric compounds showed their high efficiency in the model of staphylococcal sepsis in mice and a fairly good tolerability. ED50 values were 1.09 mg/kg for LCTA-2701 compound and 18.27 mg/kg for LCTA-2841 compound, and their chemotherapeutic index was, respectively, 22.2 and 2.3. |
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| ISSN: | 0235-2990 |