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

Mohamed Rbaa, Asmaa Oubihi, El Hassane Anouar, Mohamed Ouhssine, Faisal Almalki, Taibi Ben Hadda, Abdelkader Zarrouk, Brahim Lakhrissi

Research output: Contribution to journalArticlepeer-review

38 Scopus citations

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.

Original languageEnglish
Article number100306
JournalChemical Data Collections
Volume24
DOIs
StatePublished - Dec 2019

Keywords

  • Antibacterial activity
  • Drug design
  • Organic synthesis
  • POM analyses

Fingerprint

Dive into the research topics of 'Synthesis of new heterocyclic systems oxazino derivatives of 8-Hydroxyquinoline: Drug design and POM analyses of substituent effects on their potential antibacterial properties'. Together they form a unique fingerprint.

Cite this