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Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
ISSN: 1596-5996
EISSN: 1596-9827
Vol. 14, No. 7, 2015, pp. 1265-1272
Bioline Code: pr15166
Full paper language: English
Document type: Research Article
Document available free of charge

Tropical Journal of Pharmaceutical Research, Vol. 14, No. 7, 2015, pp. 1265-1272

 en Synthesis and Antimicrobial Activity of Some 2-Amino-4-(7- Substituted/Unsubstituted Coumarin-3-yl)-6- (Chlorosubstitutedphenyl) Pyrimidines
Imran, Mohd; Abida & Khan, Suroor Ahmad

Abstract

Purpose: To prepare some 2-amino-4-(7-substituted/unsubstitutedcoumarin-3-yl)-6-(chlorosubstitute dphenyl) pyrimidines as antimicrobial agents.
Methods: Some 2-amino-4-(7-substituted/unsubstitutedcoumarin-3-yl)-6-(chlorosubstitutedphenyl) pyrimidines were prepared by reacting 3-chlorosubstitutedphenyl-1-(7-substituted/unsubstituted coumarin-3-yl)prop-2-ene-1-ones with guanidine carbonate. The chemical structures of the synthesized compounds were elucidated by Fourier transform infra-red spectroscopy (FTIR), 1H-nuclear magnetic resonance (1H-NMR), mass spectrometry and elemental analysis. The synthesized compounds were investigated for their antimicrobial activity against four bacteria and five fungi by serial plate dilution method using ofloxacin and ketoconazole as reference antimicrobial drugs, respectively, and their minimum inhibitory concentrations (MICs) were determined.
Results: Compounds 1 (p < 0.0001), 2 (p < 0.0001), 6 (p < 0.0001) and 8 (p < 0.0001) were the most active antibacterial agents among the synthesized compounds compared to control and standard agents. Structure-activity relationship revealed that substitution of chlorine atoms at 2- and 6- positions of the phenyl ring are critical for antibacterial activity in the case of dichlorophenyl derivatives, while for monochlorophenyl derivatives, the positions 2 and 4 of the phenyl ring were critical for antibacterial activity. None of the compounds exhibited comparable antifungal activity to the standard antifungal drug, ketoconazole, even at high concentrations.
Conclusion: It is evident that the synthesized compounds are relatively very active antibacterial agents but are weak antifungal agents. However, these compounds need further evaluation of their antibacterial activity against other bacterial strains to ascertain their broad spectrum antibacterial activity.

Keywords
Pyrimidine; Coumarin; Antibacterial; Antifungal; Structure-activity relationship

 
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