Synthesis of new heterocyclic systems oxazino derivatives of 8-Hydroxyquinoline: Drug design and POM analyses of substituent effects on their potential antibacterial properties

Abstract

Abstract To remedy the problem of microbes, humanity has proposed that the use of antibiotics becomes indispensable. In this work, we present six organic compounds derivatives of 8-hydroxyquinoline newly synthesized and characterized by the usual spectroscopic methods. These compounds have been tested as antibacterial agents against six pathogenic strains, namely: E. cloacae, E. coli, K. pneumoniae, P. aeruginosa, S. aureus and A. baumanii. The minimal inhibitory concentrations were calculated and compared with three standard antibiotics (Penicillin G, Norfloxacin, and Erythromycin) by the disk diffusion technique against all used bacterial strains. The results of bioinformatics POM (Petra/Osiris/Molinspiration) bioinformatic analyses show that all compounds exhibited good bioavailability, and less toxicity profiles when compared with Penicillin G. Furthermore, drug likeness analysis suggests that the synthesized 8-hydroxyquinoline derivatives require serious transformation in order to obtain appropriate oral absorption and brain penetration for potential therapeutic applications.