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Mechanochemical synthesis of antifungal bis(benzoxaboroles).


ABSTRACT: Several piperazine bis(benzoxaboroles) have been obtained both in solution as well as in the solid state. The environmentally friendly mechanochemical approach - hitherto not applied for the preparation of benzoxaboroles - was particularly beneficial in the case of two products afforded in low yields in solution. The in vitro studies showed high potential of the studied bis(fluorobenzoxaboroles) as antifungal agents, highlighting also the influence of the fluorine substituent position on their microbiological activity. The highest activity against A. niger, A. terreus, P. ochrochloron, C. tenuis and C. albicans was displayed by the analogue of the known benzoxaborole antifungal drug Kerydin® (Tavaborole).

SUBMITTER: Borys KM 

PROVIDER: S-EPMC9057134 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature

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Mechanochemical synthesis of antifungal bis(benzoxaboroles).

Borys Krzysztof M KM   Wieczorek Dorota D   Tarkowska Magdalena M   Jankowska Agnieszka A   Lipok Jacek J   Adamczyk-Woźniak Agnieszka A  

RSC advances 20201007 61


Several piperazine bis(benzoxaboroles) have been obtained both in solution as well as in the solid state. The environmentally friendly mechanochemical approach - hitherto not applied for the preparation of benzoxaboroles - was particularly beneficial in the case of two products afforded in low yields in solution. The <i>in vitro</i> studies showed high potential of the studied bis(fluorobenzoxaboroles) as antifungal agents, highlighting also the influence of the fluorine substituent position on  ...[more]

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