Synthesis of potential efflux pump inhibitors

Abstract

Microorganisms are playing an important role at a global scale, directly affecting the environment. Antimicrobial resistance is a worldwide problem in human and veterinary medicine. It occurs when micro-organisms evolve resistance to antimicrobial substances and seems to be inevitable. The appearance of multiple resistant bacteria of human and veterinary origin is accelerated due to the inappropriate or excessive use of antimicrobials. There are different solutions proposed to solve this problem. The environment contains a lot of man-made products. Such contamination is increasing and spreading into the environment. The major bacterial solution to toxic challenges takes the form of multiple pumping systems that prevent intracellular accumulation of bactericidal and bacteriostatic substances. The ability to pump antimicrobials out of cells is a common feature of most environmental microorganisms. That’s why is very important to discover molecules inhibiting the efflux pumps also to reveal the inhibition mechanisms of it. There is a possibility to discover substances competing with antibiotics for the interaction with efflux pumps. Antibiotic treatment in combinations with such inhibitory compounds is being widely discussed. Derivatives of carbazole could be considered as potential efflux pump inhibitors or substrates. Carbazoles are heterocyclic compounds with two benzene rings linked in a tricyclic system through nitrogen atom and also could be employed as biologically active compounds. Such derivatives could be employed as antibacterial, antiviral, anti-inflammatory, anticancer, sedatives or tranquilizers agents. The slight change in the structure of these compounds causes distinguishable difference in their biological activities.[...]