engleski

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

Small heteroaromatic molecules, like nitrogen and sulphur-containing heterocycles play an extremely important role in medicinal chemistry due to variety of their possible chemical, pharmacological and industrial applications. These molecules are widely incorporated in the structure of numerous natural or synthetic medical and biochemical molecules.[1] Benzimidazoles and benzothiazoles, as one of the privileged sub- structures and an important bioactive heterocyclic building block in medicinal chemistry, while benzothiophene skeleton is incorporated in the structure of numerous therapeutic agents.[2] Herein, we present the synthesis and biological evaluation of novel nitro and amino substituted 2- benzimidazolyl and 2-benzothiazolyl benzo[b]thieno-2-carboxamides.[3] Antibacterial activity was assessed against Gram-positive and Gram-negative bacteria and the highest antibacterial activity was observed for the nitro and amino substituted benzimidazole derivatives with MICs in the range of 2-8 µg/mL. Additionally, the tested compounds not displaying promising antibacterial activity were further tested for the antiproliferative activity in vitro against three human cancer cell lines. The most pronounced and selective antiproliferative activity against MCF-7 cell line was demonstrated by amino substituted hydrochloride salt of benzothiazole derivative with an IC50 of 0.04 M.

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

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