Evaluation of the antimicrobial and fungicidal activity of nucleoside derivatives

¹ Institute of Ecology, Biotechnology and Nature Management, Kazan (Volga region) Federal University, 420008 Kazan, Russia
² Institute of Fundamental Medicine and Biology, Kazan (Volga region) Federal University, 420008 Kazan, Russia

¹ Corresponding author: Pavel.Zelenikhin@kpfu.ru

Abstract

On the background of the growing antibiotic resistance problem, the search for new antimicrobial therapy agents is of special interest. As sources of such compounds, it is reasonable to consider substances with other known target activity, like antiviral, and even the “waste heaps” content left from research on their development. In this study, we evaluated the antimicrobial, antibiofilm, mutagenic and cytotoxic properties of 83 nucleosides derivatives. All investigated agents did not inhibit the growth of E. coli ATCC 25922, S. typhimurium TA 100, S. aureus ATCC 35591, S. epidermidis, did not show any cytotoxicity towards A549 cells in MTT test, but 20 of them had a confirmed ability to inhibit the growth of C. albicans. 11 agents tested suppressed the development of C. albicans biofilms, and 5 caused the disruption of preformed yeast biofilms. The most active was compound 202, an N6-substituted adenosine derivative with a furan moiety (MIC = 32 µg/mL; BPC = 8 µg/mL). There was no mutagenic activity in the agents studied except for compounds 384 and 392. The results obtained indicate the possibility of nucleosides derivatives application as agents for the Candida species biofilm control.