0000000000390513
AUTHOR
Magdalena Tarkowska
Synthesis, structure, properties and antimicrobial activity of para trifluoromethyl phenylboronic derivatives
The [2-formyl-4-(trifluoromethyl)phenyl]boronic acid as well as its benzoxaborole and bis(benzoxaborole) derivatives were obtained and their properties studied. The 2-formyl compound displays an unusual structure in the crystalline state, with a significant twist of the boronic group, whereas in DMSO solution it tautomerizes with formation of a cyclic isomer. All the studied compounds exhibit relatively high acidity as well as a reasonable antimicrobial activity. Docking studies showed interactions of all the investigated compounds with the binding pocket of Candida albicans LeuRS. High activity against Bacillus cereus was determined for the 2-formyl compound as well as for the novel bis(be…
Mechanochemical synthesis of antifungal bis(benzoxaboroles)
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…
CCDC 2082738: Experimental Crystal Structure Determination
Related Article: Agnieszka Adamczyk-Wo��niak, Magdalena Tarkowska, Zofia Lazar, Ewa Kaczorowska, Izabela D. Madura, Anna Maria D��browska, Jacek Lipok, Dorota Wieczorek|2021|Bioorg.Chem.|119|105560|doi:10.1016/j.bioorg.2021.105560