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SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 5-PHTHALATE AND 5-GLUTARATE DERIVATIVES OF MILBEMYCINS A3/A4

J. Lugiņina, Ē. Bizdēna, A. Leonciks, V. Kumpiņš, I. Grīnšteine, M. Turks
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Abstract


Naturally occurring 16-membered macrolides milbemycins A3 and A4 were selectively esterified at their 5-OH group with phthalic and glutaric anhydrides. The obtained monoesters were further functionalized by amide formation. Propargylamide derivatives were demonstrated to undergo 1,2,3-triazole formation upon treatment with organic azides in the presence of copper catalyst. Some of the synthesized compounds exhibited useful levels of antibacterial properties against Staphylococcus aureus and Staphylococcus epidermidis.

How to Cite
Lugiņina, J.; Bizdēna, Ē.; Leonciks, A.; Kumpiņš, V.; Grīnšteine, I.; Turks, M. Chem. Heterocycl. Compd. 2015, 50, 1404. [Khim. Geterotsikl. Soedin. 2014, 1528.]

For this article in the English edition see DOI 10.1007/s10593-014-1604-2


Keywords


milbemycin A3; milbemycin A4; antibacterial activity; Staphylococcus aureus; Staphylococcus epidermidis

Full Text: PDF Supplementary File(s): Supporting information (3MB)


 

 

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