Experimental and theoretical evaluation of two indol-steroid-cyclobuta-imidazole derivatives as antibacterial drugs

Abstract

There some for treatment of infectios deseasses; however, some drugs can induce several adverse effects. The aim of this study was synthesizing and to determinate the antibacterial activity of two indol-steroid-cyclobuta-imidazole complex (compound 11 and 12) against Staphylococcus aureus, Escherichia colli and Klebsiella pneumoniae in a minimum inhibitory concentration (MIC) model, using gentamicin, ciprofloxacin, cefotaxime as controls. The following stage involved the theoretical evaluation of the interaction of both compounds 11 and 12 with the β-lactamase enzyme (5f1g) using a docking software. The data found indicate that compound 12 decrease the growth bacterial of Staphylococcus aureus, Escherichia colli and Streptococcus pneumoniae in comparison with the compound 11 and this effect only was similar to cefotaxime Other theoretical data indicated that compound 12 could interact with different type of amino acids residues such as Ser61, Leu116, Gln117, Asp120, Tyr147, Asn149, Ser209, Tyr218, Thr318, Asn342 involved in the surface of 5f1g compared with 11. These data indicate that; i) the steroid derivative (12) show better affinity by the 5f1g protein in comparison with compound 11 which is translated as higher antibacterial activity; ii) this compound is particularly interesting because could constitute a novel therapy as antibacterial agent.