Antibacterial Activity of the Halogen- and Nitro Derivatives of Benzimidazole Against <i>Bacillus Subtilis</i>

Abstract

Background. Antibiotic resistance of bacteria is a serious concern for modern medicine. The search for new compounds with a pronounced antibacterial effect is an urgent task of pharmaceutical chemistry. The aim of the study was to assess nfluence of the structure of benzimidazole and its derivatives the ability to inhibit the growth of gram-positive bacteria Bacillus subtilis. Materials and methods. Antibacterial activity of diazaheterocycles was evaluated by the method of serial dilutions. Сoncentrations from 0,06 to 1000 µg/l were used. Тhe minimum inhibitory concentration (MIC) of benzimidazole derivatives against Bacillus subtilis BKM B-407 was determined. The antibacterial effect of the studied halogen- and nitrobenzimidazoles was compared with the antimicrobial activity of benzimidazole. Results. The antimicrobial activity of the 12 benzimidazole derivatives was established. 2-trifluoromethylbenzimidazoles containing halogen atoms in the phenylene fragment had the most pronounced inhibitory effect. The dihalogenated derivatives exhibited greater antibacterial activity than the compounds with one halogen atom in the benzene ring. 5,6-dibromo-2-(trifluoromethyl)benzimidazole was the most active compound with an MIC of 0.49 µg/mL, comparable to the commercial antibiotic tetracycline. The antibacterial activity of erythromycin is a half that of this substance. Conclusions. Polyhalogen derivatives of benzimidazole are promising compounds for the development of new antimicrobial drugs against Gram-positive bacteria.

Antimicrobial properties of chlorophyll and hemin incorporated into the polymeric matrix of poly-N-vinylpyrrolidone

“…In recent years, the increasing number of microorganisms resistant to antibiotics and disinfectants poses a serious and global problem [1,2]. Thus, the urgent task is not only the search and implementation of new drugs, but also the use of such approaches as the application of photodynamic (PDT) and light-independent therapy.…”

Regioselectivity of 9-chloropyrido[1,2-a]benzimidazole halogenation reaction

“…According to numerous experimental data, introduction of halogen atoms into azaheterocyclic systems show enhancing of their biological activity [7][8][9]. For example, the paper [7] shows increasing in the number of halogen atoms in an azagetheroaromatic system enhanced the antimicrobial effect and also decreased the value of the minimum inhibitory concentration. Also, [9] reported a two or more fold decrease in the required concentration for inhibition of fungal cultures in the presence of halogens in the compound structure.…”