Synthesis and Antibacterial Activity of ll-O-(Benzoxaborole-Aminoalkylcarbamoyl) Derivatives of Macrolide Antibiotic Azithromycin
Abstract
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.
About the Authors
S. S. Printsevskaya
Gause Institute of New Antibiotics
Russian Federation
Russian Federation
A. M. Korolev
Gause Institute of New Antibiotics
Russian Federation
Russian Federation
Yu. N. Luzikov
Gause Institute of New Antibiotics
Russian Federation
Russian Federation
E. P. Mirchink
Gause Institute of New Antibiotics
Russian Federation
Russian Federation
E. B. Isakova
Gause Institute of New Antibiotics
Russian Federation
Russian Federation
A. N. Tevyashova
Gause Institute of New Antibiotics; D. Mendeleev University of Chemical Technology of Russia
Russian Federation
Russian Federation
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Review
For citations:
Printsevskaya S.S., Korolev A.M., Luzikov Yu.N., Mirchink E.P., Isakova E.B., Tevyashova A.N. Synthesis and Antibacterial Activity of ll-O-(Benzoxaborole-Aminoalkylcarbamoyl) Derivatives of Macrolide Antibiotic Azithromycin. Antibiot Khimioter = Antibiotics and Chemotherapy. 2018;63(1-2):3-7. (In Russ.)
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