Abstract
Purpose: To prepare and evaluate some 2-piperidinomethylamino-4-(7-H/substitutedcoumarin-3-yl)-6- chlorosubstitutedphenyl pyrimidines as antimicrobial agents.Methods: Some 2-piperidinomethylamino-4-(7-H/substitutedcoumarin-3-yl)-6-chlorosubstitutedphenyl pyrimidines were prepared by reacting 2-amino-4-(7-H/substitutedcoumarin-3-yl)-6- (chlorosubstitutedphenyl) pyrimidines with piperidine and formaldehyde. The chemical structures of the synthesized compounds were elucidated by Fourier transform infrared (FTIR), 1H-nuclear magnetic resonance (1H-NMR), mass spectrometry and elemental analysis. These compounds were investigated for their antimicrobial activity against ten bacteria and five fungi by serial plate dilution method using standard drugs, namely, ofloxacin and ketoconazole, respectively, and their minimum inhibitory concentrations (MICs) were also determined.Results: A total of eighteen new compounds (1a-18a) were synthesized. Compound 6a (MIC = 50 μg/mL; p < 0.05 or less) displayed the highest activity against S. aureus, E. faecalis, S. epidermidis, B. subtilis, and B. cereus. Compound 6a further showed good activity (MIC = 25 μg/mL; p < 0.05 or less) against E. coli; P. aeruginosa K. pneumonia, B. bronchiseptica, and P. vulgaris. Compounds 6a (MIC = 25 μg/mL; p < 0.0001) and 17a (MIC = 25 μg/mL; p < 0.0001) displayed very good activity against C. albicans, A. niger, A. flavus, M. purpureous, and P. citrinum, respectively. Analysis of structure-activity relationship revealed that the presence of bromo group at 7-postion of the coumarin moiety along with the 4-chlorophenyl group at position-6 of the pyrimidine ring is critical for antimicrobial activity against Gram-positive bacteria, Gram negative bacteria and fungi.Conclusion: The synthesized 2-piperidino derivatives are better antifungal and antibacterial agents than the earlier reported 2-morpholino derivatives, but require further investigations against other microbial strains to ascertain their broad spectrum antimicrobial activity.Keywords: Pyrimidine, Coumarin, Piperidine, Antibacterial, Antifungal, Structure activity relationship
Highlights
Microbial infections have been creating problems for mankind since centuries and scientists have developed a large number of antimicrobial agents for the treatment of these infections
Because of the Encouraged by these observations and in development of antibiotic resistance and continuation of our search for potent emergence of new microbial diseases, there is a antimicrobial agents [21,22] including need to develop new antimicrobial agents for the antimicrobial agents having coumarin moiety [23
Pyrimidine derivatives have an important place in rin-3-yl)-6-chlorosubstitutedphenyl pyrimidines, medicinal chemistry as these are associated with after the title compounds (1a-18a), as a broad range of biological activities [2,3,4,5,6,7] antimicrobial agents
Summary
Microbial infections have been creating problems for mankind since centuries and scientists have developed a large number of antimicrobial agents for the treatment of these infections. Because of the Encouraged by these observations and in development of antibiotic resistance and continuation of our search for potent emergence of new microbial diseases, there is a antimicrobial agents [21,22] including need to develop new antimicrobial agents for the antimicrobial agents having coumarin moiety [23-. Pyrimidine derivatives have an important place in rin-3-yl)-6-chlorosubstitutedphenyl pyrimidines, medicinal chemistry as these are associated with after the title compounds (1a-18a), as a broad range of biological activities [2,3,4,5,6,7] antimicrobial agents. The antimicrobial activity of pyrimidine derivatives against broad range of microbes makes it an important skeleton in medicinal chemistry and drug development against microbes. A number of piperidine ring containing chemical compounds have been reported as antimicrobial agents [17,18,19,20]
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