Synthesis and antimicrobial activity of 4-trifluoromethylpyridine nucleosides

Shaikha S. Alneyadi; Anas A. Abdulqader; Alaa A. Salem; Ibrahim M. Abdou

doi:10.1515/hc-2017-0019

Synthesis and antimicrobial activity of 4-trifluoromethylpyridine nucleosides

Shaikha S. Alneyadi, Anas A. Abdulqader, Alaa A. Salem, Ibrahim M. Abdou

Department of Chemistry

Research output: Contribution to journal › Article › peer-review

6 Citations (Scopus)

Abstract

4-Trifluoromethylpyridine derivatives 4-8 represent good candidates for the discovery of new antibacterial agents. Fluorinated pyridine nucleosides 4-7 and non-nucleoside analogues 8a,b were synthesized and evaluated for their antibacterial activities against Staphylococcus aureus, Bacillus infantis, Escherichia coli and Stenotrophomonas maltophilia. The minimum inhibitory concentrations (MICs) of the new nucleosides 4-7 range from 1.3 to 4.9 μg/mL and MICs of fluoroaryl derivatives 8a,b are in the range of 1.8-5.5 μg/mL. Activity of amoxicillin, the reference drug, is 1.0-2.0 μg/mL under similar conditions.

Original language	English
Pages (from-to)	197-203
Number of pages	7
Journal	Heterocyclic Communications
Volume	23
Issue number	3
DOIs	https://doi.org/10.1515/hc-2017-0019
Publication status	Published - Jun 2017

Keywords

Antimicrobial
Fluoropyridine
Nucleosides
Synthesis
gHMBC

ASJC Scopus subject areas

Organic Chemistry

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10.1515/hc-2017-0019

Cite this

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title = "Synthesis and antimicrobial activity of 4-trifluoromethylpyridine nucleosides",

abstract = "4-Trifluoromethylpyridine derivatives 4-8 represent good candidates for the discovery of new antibacterial agents. Fluorinated pyridine nucleosides 4-7 and non-nucleoside analogues 8a,b were synthesized and evaluated for their antibacterial activities against Staphylococcus aureus, Bacillus infantis, Escherichia coli and Stenotrophomonas maltophilia. The minimum inhibitory concentrations (MICs) of the new nucleosides 4-7 range from 1.3 to 4.9 μg/mL and MICs of fluoroaryl derivatives 8a,b are in the range of 1.8-5.5 μg/mL. Activity of amoxicillin, the reference drug, is 1.0-2.0 μg/mL under similar conditions.",

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AU - Alneyadi, Shaikha S.

AU - Abdulqader, Anas A.

AU - Salem, Alaa A.

AU - Abdou, Ibrahim M.

PY - 2017/6

Y1 - 2017/6

N2 - 4-Trifluoromethylpyridine derivatives 4-8 represent good candidates for the discovery of new antibacterial agents. Fluorinated pyridine nucleosides 4-7 and non-nucleoside analogues 8a,b were synthesized and evaluated for their antibacterial activities against Staphylococcus aureus, Bacillus infantis, Escherichia coli and Stenotrophomonas maltophilia. The minimum inhibitory concentrations (MICs) of the new nucleosides 4-7 range from 1.3 to 4.9 μg/mL and MICs of fluoroaryl derivatives 8a,b are in the range of 1.8-5.5 μg/mL. Activity of amoxicillin, the reference drug, is 1.0-2.0 μg/mL under similar conditions.

AB - 4-Trifluoromethylpyridine derivatives 4-8 represent good candidates for the discovery of new antibacterial agents. Fluorinated pyridine nucleosides 4-7 and non-nucleoside analogues 8a,b were synthesized and evaluated for their antibacterial activities against Staphylococcus aureus, Bacillus infantis, Escherichia coli and Stenotrophomonas maltophilia. The minimum inhibitory concentrations (MICs) of the new nucleosides 4-7 range from 1.3 to 4.9 μg/mL and MICs of fluoroaryl derivatives 8a,b are in the range of 1.8-5.5 μg/mL. Activity of amoxicillin, the reference drug, is 1.0-2.0 μg/mL under similar conditions.

KW - Antimicrobial

KW - Fluoropyridine

KW - Nucleosides

KW - Synthesis

KW - gHMBC

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Synthesis and antimicrobial activity of 4-trifluoromethylpyridine nucleosides

Abstract

Keywords

ASJC Scopus subject areas

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