TY - JOUR
T1 - Synthesis of new heterocyclic systems oxazino derivatives of 8-Hydroxyquinoline
T2 - Drug design and POM analyses of substituent effects on their potential antibacterial properties
AU - Rbaa, Mohamed
AU - Oubihi, Asmaa
AU - Anouar, El Hassane
AU - Ouhssine, Mohamed
AU - Almalki, Faisal
AU - Hadda, Taibi Ben
AU - Zarrouk, Abdelkader
AU - Lakhrissi, Brahim
N1 - Publisher Copyright:
© 2019 Elsevier B.V.
PY - 2019/12
Y1 - 2019/12
N2 - 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.
AB - 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.
KW - Antibacterial activity
KW - Drug design
KW - Organic synthesis
KW - POM analyses
UR - http://www.scopus.com/inward/record.url?scp=85074790645&partnerID=8YFLogxK
U2 - 10.1016/j.cdc.2019.100306
DO - 10.1016/j.cdc.2019.100306
M3 - Article
AN - SCOPUS:85074790645
SN - 2405-8300
VL - 24
JO - Chemical Data Collections
JF - Chemical Data Collections
M1 - 100306
ER -