Effects of Diborolane Containing Oxo/Amine Compounds on Clinically Important Bacteria and Candida Species

Abstract

A good yield of 1,2-diborolanderivatives 2-8 was obtained from the reaction of 1,2-dichloro-1,2-diborolane 1 and R2NLi/ArNHLi/PhOLi/H2O. The structures of these new derivatives were characterized by nuclear magnetic resonance spectroscopy. The molecular structures of 4 and 7a were also determined using single-crystal X-ray diffraction. The antimicrobial activities of synthesized compounds were tested against clinically important Gram-positive, Gram-negative bacteria, and Candida species. The most effective substances were found to be compounds 2, 3, 4, 6 and 8 among the tested compounds. Therefore, the activity of these substances were investigated against Staphylococcus aureus ATCC 43300 and Enterococcus faecalis ATCC 51575, which form biofilms and have antibiotic resistance. Compound 2, 6 and 8 appears to be a promising candidate for potential antibacterial agents against these bacterial strains, especially given its potent activity against biofilm-forming and antibiotic resistant strains. The results indicate that these new materials will be evaluated as potential drugs against infectious diseases in the future. © 2024 Elsevier B.V.