Abstract

Uncontrolled use of antimicrobial drugs leads to the selection and spread of resistant strains of microorganisms. Рhosphonium compounds and their derivatives have been chosen as very perspective during searching of new highly active antimicrobial and antiseptic drugs. Objective. To study antimicrobial action of some new condensed polynuclear arens at broad spectrum of reference cultures. Materials and methods. The phosphonium salt and its derivatives from the condensed polynuclear arens were studied. Fourteen reference cultures of Gram-positive and Gram-negative bacteria from different taxonomic position and culture of yeast fungi genus Candida were used. Antimicrobial activity of the test substances was studied with micromethod with disposable polystyrene plates and Takachi microtitrator. Results. Phosphonium salt and it derivatives based on the condensed polynuclear arenes have high antimicrobial activity. The derivatives of phosphonium salt based on the condensed polynuclear arens (compound II) show the highest antimicrobial activity against Gram-positive microorganisms ( S. aureus 209, M . luteus ATCC 3941, and non-spore forms B. cereus ATCC 10702). The minimal inhibitory concentrations of this compound were 0,48 mcg/ml, 0,03 mcg/ml and 0,24 mcg/ml respectively. Less active antibacterial activity showed compound I. Its’ minimal inhibitory concentrations (MIC) were 1,95 mcg/ml against Gram-positive microorganisms ( S. aureus and 209 M . luteus ATCC 3941 and vegetative cells of spore-forming bacillus – B. cereus ATCC 10702). Both compounds have shown moderate antimicrobial activity against Gram-negative microorganisms. Minimum inhibitory concentrations were in range from 31,2 to 125 mcg/ml. Phosphonium salt and its derivative based on condensed polynuclear arenes, that were studied, exhibit moderate antifungal activity against C. utilis LIA - 01 (MIC of compound I was 31,2 mcg/ml, compound II – 7,8 mcg/ml; MFtC of compound I - 62,5 mcg/ml, compound II– 15,6 mcg/ml). Conclusions: It was established that phosphonium salt and its derivative based on the condensed polynuclear arenes, that were studied, demonstrated the highest antimicrobial activity against gram-positive microorganisms. The compound II demonstrates higher antimicrobial activity than compound I. Both tested compounds showed moderate antimicrobial activity against gram-negative bacteria and yeast fungi from the Candida genus .

Highlights

  • Antimicrobial activity of the test substances was studied with micromethod with disposable polystyrene plates and Takachi microtitrator

  • Phosphonium salt and derivatives based on the condensed polynuclear arenes have high antimicrobial activity

  • The derivatives of phosphonium salt based on the condensed polynuclear arens show the highest antimicrobial activity against Gram-positive microorganisms (S. aureus 209, M. luteus ATCC 3941, and non-spore forms B. cereus ATCC 10702)

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Summary

Introduction

ЇЇ мінімальні інгібуючі концентрації стосовно грампозитивних (S. aureus 209, M. luteus АТСС 3941) бактерій були 0,48 мкг/мл і 0,03 мкг/мл відповідно, а щодо вегетативних клітин спороутворювальних бацил (B. cereus ATCC 10702) – 0,24 мкг/мл. ЇЇ мінімальні інгібуючі концентрації дорівнювали 1,95 мкг/мл стосовно грампозитивних мікроорганізмів (S. aureus 209 і M. luteus ATCC 3941 і вегетативних клітин спороутворювальних бацил B. cereus ATCC 10702). Досліджувані фосфонієва сіль та її похідна на основі багатоядерних конденсованих аренів виявили помірну протигрибкову активність стосовно C. utilis ЛИА-01 (МІК сполуки I дорівнює 31,2 мкг/мл, а сполуки II – 7,8 мкг/мл і МФцК сполуки I становить 62,5 мкг/мл, а сполуки II – 15,6 мкг/мл).

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