Synthesis and Antibacterial Activity of ll-O-(Benzoxaborole-Aminoalkylcarbamoyl) Derivatives of Macrolide Antibiotic Azithromycin
Benzoxaborole, a structure in medicinal chemistry privileged due to its desirable physicochemical and drug-like properties, was used for the synthesis of azithromycin-benzoxaborole conjugates in which benzoxaborole fragment was attached to the 11-hydroxy group of the antibiotic via aminoalkylcarbomo...
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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/62 |
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| Summary: | Benzoxaborole, a structure in medicinal chemistry privileged due to its desirable physicochemical and drug-like properties, was used for the synthesis of azithromycin-benzoxaborole conjugates in which benzoxaborole fragment was attached to the 11-hydroxy group of the antibiotic via aminoalkylcarbomoyl spacer. The obtained hybrids 5-7 demonstrated wide spectrum of antibacterial activity, especially against susceptible S.pneumonia strain although the investigated modification didn't result in overcoming bacterial resistance in MRSA. |
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| ISSN: | 0235-2990 |