Arzneimittelforschung 2001; 51(5): 420-424
DOI: 10.1055/s-0031-1300057
Antibiotics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

Synthesis of Some Benzimidazole Derivatives and their Antibacterial and Antifungal Activities

Hasan Küçükbav
a   Department of Chemistry, Faculty of Arts and Sciences, İnönü University, Malatya, Turkey
,
Riza Durmaz
b   Department of Microbiology Faculty of Medicine, İnönü University, Malatya, Turkey
,
Mine Güven
a   Department of Chemistry, Faculty of Arts and Sciences, İnönü University, Malatya, Turkey
,
Selami Günal
b   Department of Microbiology Faculty of Medicine, İnönü University, Malatya, Turkey
› Author Affiliations
Further Information

Publication History

Publication Date:
26 December 2011 (online)

Summary

A number of new benzimidazole derivatives were synthesized by the reaction of benzimidazole with appropriate alkyl hal-ides. The compounds synthesized were intentified by 1H-ΝΜR, Fourier Transformation Infrared (FT-IR) and micro analysis. All new and related compounds studied in this work were screened for their in vitro antimicrobial activities against the standard strains: Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 29213), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and the yeasts Candida albicans and Candida tropicalis. Eleven of the compounds were found effective to inhibit the growth of Gram-pos itive bacteria (E. faecalis and S. aureus) at MIC values between 12.5-400 μg/ml. None of the compounds exhibited antimicrobial activity against Gram-negative bacteria (E. coli and P. aeruginosa) at the concentrations studied (6.25-800 µg/ml). All compounds (except compound 3) were significantly effective against C. tropicalis with MIC values of 6.25-400 µg/ ml. Eight of the tested compounds showed an antifungal activity against C. albicans with a range of the MICs between 50 and 400 µg/ml.

Zusammenfassung

Synthese von Benzimidazol-Derivaten und ihre antibakterielle und antimykotische Aktivität

Neue Benzimidazol-Derivate wurden durch die Reaktion von Benzimidazol mit entsprechenden Alkylhaliden synthetisiert. Die Substanzen wurden mittels 1H-NMR Fourier Transform Infrarot (FT-IR) und anderen spektroskopischen Methoden sowie mittels Microanalyse identifiziert. Alle in dieser Arbeit untersuchten Substanzen wurden auf ihre antimicrobielle Wirkung gegenüber Standardkeimen in vitro geprüft: Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 29213), Eschericha coli (ATCC 25922), Pseudomanas aeruginosa (ATCC 27853) und gegen Candida albicans und Candida tropicali. Bei 11 der untersuchten Substanzen wurde eine Hemmung des Wachstums der Gram-positiven Bakterien E. faecalis und S. aureus bei Hemmkonzentration von 12.5-800 μg/ml und eine antimikrobielle Wirkung gegenüber den Gram-negativen Bakterien E. coli und P. aeruginosa beobachtet. Alle Verbindungen (außer Verbindung 3) waren alle signifikant wirksam gegen C. tropicalis bei MHK-Werten (mittlere Hemmkonzentration) von 6.25-400 μg/ml. Acht der getesteten Verbindungen zeigten antimykotische Wirkung gegen C. albicanis mit einer MHK (mittlere Hemmkonzentration) zwischen 50 und 400 μg/ml.