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Journal of Applied Sciences and Environmental Management
World Bank assisted National Agricultural Research Project (NARP) - University of Port Harcourt
ISSN: 1119-8362
Vol. 22, No. 7, 2018, pp. 1121-1127
Bioline Code: ja18190
Full paper language: English
Document type: Research Article
Document available free of charge

Journal of Applied Sciences and Environmental Management, Vol. 22, No. 7, 2018, pp. 1121-1127

 en Double Alkynylation of Quinoline-5,8-diones and their In-silico and Antimicrobial Studies
EZEOKONKWO, MA; EZUGWU, JA; OKAFOR, SN; ONOABEDJE, EA; GODWIN-NWAKWASI, EU & IBEANU, FN

Abstract

A double alkynylation of quinoline-5,8-dione to furnished bis-alkynylquinoline-5,8-dione in good yields and their in silico and antimicrobial studies is described. This was achieved by cross-coupling of 6,7- dibromoquinoline-5,8-dione with various terminal alkynes in the presence of bis(triphenylphosphine) palladium(II) chloride as a pre-catalyst and tetrabutyl ammonium fluoride trihydrate. The structures of the synthesised compounds were confirmed by UV/Visible, Fourier Transform-Infrared and 1H and 13C-NMR spectral data. The synthesised compounds exhibited good activity against Escherichia Coli check for this species in other resources 1, Escherichia Coli 12, Klebsiella Pneumonia check for this species in other resources , Pseudomonas aeroginosa check for this species in other resources and Staphylococcus aureus check for this species in other resources compare to the gentamycin and ampicillin. Molecular docking simulation study of the binding interactions of compounds with receptors disclosed significant binding affinity for P. aeruginosa LpxC than the E. coli glutaredoxin.

Keywords
6, 7-Dibromoquinoline-5; 8-dione; Bis-alkynylquinoline-5,8-diones; Terminal alkynes; Antimicrobial activity.

 
© Copyright 2018 - Ezeokonkwo et al.

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