Antibacterial and Antifungal Activity of 2-S-Nitrobenzyl-Substituted Halogenobenzimidazoles

Ref ID: 18742

Author:

A. E. Laudy, PhD – Adiunct 1, E. Swietochowska, MS – Student 1, M. Kozlowska, PhD – Adiunct 2, Z. Kazimierczuk, PhD – Prof. 2, S. Tyski, PharmD – Prof.1,3;

Author address:

1Med. Univ. of Warsaw, Warsaw, Poland, 2Warsaw Univ. of Life Sci., Warsaw, Poland, 3Natl. Med.s Inst., Warsaw, Poland.

Full conference title:

52nd Annual ICAAC

Date: 9 September 2014

Abstract:

Background: One of the main reasons of therapeutic failures in the treatment of bacterial infections is the resistance of microorganisms, especially hospital strains, to a broad range of antibiotics. Therefore it is necessary to search for the new compounds active against microorganisms. Methods: The antimicrobial activity of 12 new synthesised 2-S-nitrobenzyl-substituted mono-, di-, tetra-halogenobenzimidazoles was investigated by disc-diffusion assay and MIC value determination, according to CLSI recommendation. 400 μg samples of the new benzimidazole derivatives were applied onto paper discs. The reference ATCC and NCTC strains of Gram-positive bacteria, non-fermentative Gram-negative rods, Enterobacteriaceae family and yeast as well as clinical strains were investigated. Results: The significant differences between Gram-positive and Gram-negative bacteria susceptibility to the new substituted benzimidazoles were observed. In general, all but one studied new agents were active especially against: Staphylococcus aureus (including MRSA), S. epidermidis (including MRSE), Bacillus subtilis and Geobacillus stearothermophilus – MICs ≥ 0.786 mg/L.The activity of new agents depended on the structure. All 2-S-dinitrobenzyl-substituted benzimidazoles exhibited higher activity (MICs: 0.786 – 25 mg/L) than derivatives with one NO2 group (MICs: 50 – > 200 mg/L). Moreover, di-halogenobenzimidazoles were more active against cocci than monohalogeno- substituted agents. 4,6-dichloro-2-(2,4-dinitrobenzylthio)-1H-benzimidazole exhibited the highest activity among studied agents to Staphylococcus and Bacillus strains (MICs: 0.786 – 3.125 mg/L). Interestingly, all Enterococcus spp. were no susceptible to any analysed derivatives. Conclusions: Presented data indicate the structure-activity relationships of analysed agents toward varied microorganisms. Obtained results provide the reasons for the intensive search for microbiologically active substances among new benzimidazoles. The study was supported by the Foundation for the Development of Diagnostics and Therapy, Warsaw, Poland.

Abstract Number: F-1533

Conference Year: 2012

Link to conference website: NULL

New link: NULL

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