부산대학교 도서관

We report here the synthesis of a series of different 1,2,3,4-tetrahydro- and pyrido[1,2-a]benzimidazoles and assessment of their in vitro antibacterial activity against Gram-positive (Bacillus cereus) and Gram-negative (Escherichia coli AB1157, Pseudomonas aeruginosa PAO1) bacteria. Pyrido[1,2-a]benzimidazoles were the most effective against Bacillus cereus, while 1,2,3,4-tetrahydro derivatives produced the greatest level of growth inhibition of Gram-negative (Escherichia coli AB1157) bacteria. The antibacterial activity of 2,4-dimethyl-7,8-dinitropyrido[1,2-a]benzimidazole was comparable to or exceeded the efficacy of commercial tetracycline, kanamycin, levomycetin, and erythromycin formulations. A genotoxicology test (the Allium test) was used to study the mitosis-modifying and mutagenic actions of a series of condensed azaheterocyclic compounds with marked antibacterial effects. On the basis of the antibacterial activity of some of the condensed benzimidazole derivatives containing a nodal nitrogen atom detected here and the low toxicity of similar azaheterocycles led to the conclusion that there is potential for further searches for novel antibiotics among compounds of this class. [ABSTRACT FROM AUTHOR]