A study of antimicrobial and antifungal activity of 2-((5-(2-bromophenyl)-4-substituted-4H-1,2,4-triazol-3-yl)thio)acetates

Bacteria and fungi are among the most ancient creatures found on Earth. Since the advent of medicine, humankind has always sought new means and ways to combat these microorganisms. In modern scientific society, the tendency to seek new antimicrobial and antifungal agents is only increasing. 1,2,4-triazole derivatives, among which effective drugs and new molecules have already been found, make quite an interesting platform for the creation of new antifungal and antimicrobial agents. A promising direction for the search for antimicrobial and antifungal agents are 2-((5-(2-bromophenyl)-4-substituted-4H-1,2,4-triazol-3-yl)thio)acetates.

The thirst for existence and the constant transformation of bacteria encourages scientists around the world to create new and new antimicrobials. Certainly, it is much easier to create an active molecule on an already known platform, which has proven itself as a biologically active nucleus [1][2][3][4].

Materials and methods
Antimicrobial and antifungal activity of the newly synthesized 2-((5-(2-bromophenyl)-4-substituted-4H-1,2,4-triazol-3-yl)thio)acetates was investigated with the method of serial dilutions according to guidelines [14]. The synthesized compounds were prepared by double serial dilutions, with the initial concentration of 1 mg/ml in Mueller-Hinton broth, in the volume of 1 ml. Then 0.1 ml of microbial curtain (106 μ/ml) was added. Minimum inhibitory concentration (MIC) was determined without visible growth in a test tube with a minimum concentration of the drug; the minimum bactericidal/fungicidal concentration (MBcC, MFcC) was determined without growth on agar after inoculation from transparent tubes. The synthesized compounds were dissolved in dimethylsulfoxide.

Results
As a result, the antimicrobial and antifungal activity of 14 new compounds was investigated.
The most active compounds with antifungal effect are IIf-IIh. Substances IIf-IIh and IIj, IIk have moderate antimicrobial effect to P. aeruginosae.
Some conclusions have been made regarding "structurebiological activity" dependence.
As a result of the research it should be noted that the conversion to 2-((5-(2-bromophenyl)-4-substituted-4H-1,2,4-triazol-3-yl)thio)acetate salts and the choice of dimethylammonium as cation leads to an increase in the antimicrobial and antifungal effects.
Compounds with antifungal effect are IIf-IIh. Substances IIf-IIh and IIj, IIk have moderate antimicrobial effect to P. aeruginosae. But none of the compounds surpasses the comparison drug.

Funding
The research is carried out in the framework of the research activities of Zaporizhzhia State Medical University "Synthesis, modification and study of the properties of 1,2,4-triazole derivatives aimed at creating an antimicrobial drug", state registration number 0120U101649.