engleski

Antibacterial and antiproliferative activity of novel 2-benzimidazolyl- and 2-benzothiazolyl-substituted benzo[b]thieno-2-carboxamides

Novel nitro 3a-3f and amino 4a-4f and 5a-5f substituted 2-benzimidazolyl and 2- benzothiazolyl benzo[b]thieno-2-carboxamides were designed and synthesized as potential antibacterial agents. The antibacterial activity of these compounds has been evaluated against Gram-positive (Staphylococcus aureus and Enterococcus faecalis) and Gram-negative bacteria (Escherichia coli and Moraxella catarrhalis). The most promising antibacterial activity was observed for the nitro and amino substituted benzimidazole derivatives 3a, 4a, 5a and 5b with MICs 2-8 µg/mL. Additionally, compounds with inferior antibacterial activity were further tested for their antiproliferative activity in vitro against three human cancer cell lines. Amino substituted benzothiazole hydrochloride salt 5d displayed the most pronounced and selective activity against the MCF-7 cell line with an IC50 of 40 nM. Furthermore, DNA binding experiments of selected derivatives indicated that DNA cannot be considered as a primary biological target for this type of compounds.

benzo[b]thieno-2-carboxamides ; benzimidazoles ; benzothiazoles ; antibacterial activity ; antiproliferative activity ; DNA binding

INSERM UMR-S1172, Jean-Pierre Aubert Research Centre (JPARC), Université de Lille