Synthesis, antibacterial and antitubercular activities of benzimidazole bearing substituted 2-pyridone motifs

作者: N.C. Desai , N.R. Shihory , G.M. Kotadiya , Priyanka Desai

DOI: 10.1016/J.EJMECH.2014.06.004

关键词: CytotoxicityVero cell2-PyridoneBenzimidazoleStereochemistrySelectivityMic valuesLipophilicityChemistryAntibacterial activity

摘要: Abstract A series of benzimidazole bearing 2-pyridones 5a–r were synthesized and evaluated for their in vitro antibacterial antitubercular activity. Further, all compounds examined cytotoxic study on VERO cell line characterized by well-known spectral techniques. It was observed that the 5h, 5i, 5k, 5q 5r found to possess significant broad spectrum activity (12.5–100 μg/mL MIC), while 5g-5i, 5k 5l proved be most potent in range 2.76–20.4 μM MIC at low level cytotoxicity, indicating good selectivity. From SAR studies, lipophilic profile remarkably vital activity, values could not directly correlated with lipophilicity.

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