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Synthesis, Characterization of 2-Methylthio-1, 4-Dihydropyrimidines for its Antibacterial Potential


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1 Dr. D. Y. Patil Unitech Society’s, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune-411018, India
     

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Some novel 2-methylthio-1, 4-dihydropyrimidine derivatives (II) have been prepared in good yields by alkylation of 1,2,3,4-tetrahydropyrimidines (I) with methyl iodide in the presence of pyridine. All the synthesized compounds were characterized by, IR and 1H NMR spectra, Mass spectra and by elemental analysis. The title compounds were screened for their antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Proteus vulgaris. Ampicillin was used as a standard drug for evaluating antibacterial activity. Compounds with chlorine (IIe, IIf), nitro (IIi) and 3, 4, 5-trimethoxy groups (IIj) at para position in the aryl moiety were found to have potent activity amongst other compounds. Other compounds shows moderate activity.

Keywords

2-Methylthio-1, 4-Dihydropyrimidine, Biginelli Reaction, Synthesis, Antibacterial Activity.
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  • Synthesis, Characterization of 2-Methylthio-1, 4-Dihydropyrimidines for its Antibacterial Potential

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Authors

Varsha I. Sarode
Dr. D. Y. Patil Unitech Society’s, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune-411018, India
Ritesh P. Bhole
Dr. D. Y. Patil Unitech Society’s, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune-411018, India

Abstract


Some novel 2-methylthio-1, 4-dihydropyrimidine derivatives (II) have been prepared in good yields by alkylation of 1,2,3,4-tetrahydropyrimidines (I) with methyl iodide in the presence of pyridine. All the synthesized compounds were characterized by, IR and 1H NMR spectra, Mass spectra and by elemental analysis. The title compounds were screened for their antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Proteus vulgaris. Ampicillin was used as a standard drug for evaluating antibacterial activity. Compounds with chlorine (IIe, IIf), nitro (IIi) and 3, 4, 5-trimethoxy groups (IIj) at para position in the aryl moiety were found to have potent activity amongst other compounds. Other compounds shows moderate activity.

Keywords


2-Methylthio-1, 4-Dihydropyrimidine, Biginelli Reaction, Synthesis, Antibacterial Activity.

References