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Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N -Diethyl-Substituted Amido Moieties

Ajani, Olayinka O. and Familoni, O. B. and Wu, Feipeng and Echeme, Johnbull O and Sujiang, Zheng (2012) Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N -Diethyl-Substituted Amido Moieties. International Journal of Medicinal Chemistry. pp. 1-14.

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Abstract

Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities. We have synthesized a series of α-tolylsulfonamide, 1–11 and their substituted N,N-diethyl-2- (phenylmethylsulfonamido) alkanamide derivatives, 12–22 in improved and excellent yields in aqueous medium at room temperature through highly economical synthetic routes. The chemical structures of the synthesized compounds 1–22 were confirmed by analytical and spectral data such as IR, 1H- and 13C-NMR, andmass spectra. The in vitro antibacterial activity of these compounds along with standard clinical reference, streptomycin, was investigated on two key targeted organisms. It was observed that1 (benzylsulfonyl) pyrrolidine-2-carboxylic acid, 2 emerged as the most active compound against Staphylococcus aureus at MIC value of 1.8 μg/mL while 4-(3-(diethylamino)-3-oxo 2-(phenylmethylsulfonamido) propyl) phenyl phenylmethanesulfonate, 22 was the most active sulfonamide scaffold on Escherichia coli at MIC value of 12.5 μg/mL.

Item Type: Article
Subjects: Q Science > Q Science (General)
Q Science > QD Chemistry
Divisions: Faculty of Engineering, Science and Mathematics > School of Chemistry
Depositing User: Mrs Hannah Akinwumi
Date Deposited: 26 Apr 2018 09:08
Last Modified: 26 Apr 2018 09:08
URI: http://eprints.covenantuniversity.edu.ng/id/eprint/10696

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