In vitro anti-microbial and DNA cleavage studies of benzimidazole derivatives


ABSTRACT:

The increase in bacterial resistance has attracted considerable interest in the discovery and development of new classes of antibacterial agents. The new agents should preferably consist of chemical characteristics that clearly differ from those of existing agents. Benzimidazoles are remarkably effective compounds both with respect to their bacteria inhibitory activity and their favorable selectivity ratio. Extensive biochemical and pharmacological studies have confirmed that these molecules are effective against various strains of microorganisms. Some benzimidazole compounds inhibit the biosynthesis of ergosterol, required in the cell membrane of fungi. They have antibacterial, antifungal, and antiviral activity. This ring system is present in numerous antiparasitic and antitumoral drugs. The benzimidazole structure is part of the nucleotide portion of vitamine B12 and the nucleus of some drugs, such as proton pump inhibitors and anthelmintic agents. Proton pump inhibitors (PPIs) are substituted benzimidazole derivatives that selectively and irreversibly inhibit the gastric hydrogen–potassium adenosine triphosphatase (H+K + -ATPase) pump mechanism. The antimicrobial activity of this class of compounds was investigated against Helicobacter pylori[10] and against oral streptococci. Also, benzimidazole and its derivatives are of considerable importance because of their antihistaminic, cytostatic, local analgesic, hypotensive and anti-inflammatory activity. Benzimidazole was confirmed to have moderate in vitro anti-HIV effect.

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