Synthesis and antibacterial activity of novel phosphonium salts on the basis of pyridoxine |
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| Authors: | Mikhail V Pugachev Nikita V Shtyrlin Lubov P Sysoeva Elena V Nikitina Timur I Abdullin Alfiya G Iksanova Alina A Ilaeva Rashid Z Musin Eugeny A Berdnikov Yurii G Shtyrlin |
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| Institution: | 1. Research and Educational Center of Pharmacy, Kazan Federal University, Kazan 420008, Russian Federation;2. A.E. Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Centre of the Russian Academy of Sciences, Kazan 420088, Russian Federation |
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| Abstract: | A series of 13 phosphonium salts on the basis of pyridoxine derivatives were synthesized and their antibacterial activity against clinically relevant strains was tested in vitro. All compounds were almost inactive against gram-negative bacteria and exhibited structure-dependent activity against gram-positive bacteria. A crucial role of ketal protection group in phosphonium salts for their antibacterial properties was demonstrated. Among synthesized compounds 5,6-bistriphenylphosphonio(methyl)]-2,2,8-trimethyl-4H-1,3]dioxino4,5-c]pyridine dichloride (compound 20) was found to be the most effective towards Staphylococcus aureus and Staphylococcus epidermidis strains (MIC 5 μg/ml). The mechanism of antibacterial activity of this compound probably involves cell penetration and interaction with genomic and plasmid DNA. |
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| Keywords: | Quaternary phosphonium salts Pyridoxine Antibacterial activity |
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