Abstract
A series of novel 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one aliphatic/ aromatic/ heterocyclic amine derivatives were synthesized in good yield. The synthesized compounds were characterized by 1H-NMR, FTIR and elemental analysis. All the synthesized compounds were screened for their in vitro antibacterial activity by agar well diffusion and micro dilution method against standard strains of Gram-Positive (Bacillus Subtilis MTCC 121 and Staphylococcus epidermidis 435), and Gram-negative (Xanthomonas Campestris 7903 and Pseudomonas aeruginosa MTCC 7908) bacteria. Compounds with substituted heterocyclic piperazine moiety showed good activity. In particular, compound 6i showed two fold better activity compared to the standard drug Strepyomycin sulphate.
Keywords: 2-Aminopyridine, Antibacterial activity, Aromatic amines, Phosphorousoxychloride, Reduction, Strepyomycin
Medicinal Chemistry
Title:Synthesis of 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2- a] pyrimidin-4-one Derivatives as Antibacterial Agents
Volume: 9 Issue: 2
Author(s): Byregowda Krishnamurthy, Kambappa Vinaya, Devraj Rakshith, Doddakunche Shivaramu Prasanna and Kanchugarakoppal Subbegowda Rangappa
Affiliation:
Keywords: 2-Aminopyridine, Antibacterial activity, Aromatic amines, Phosphorousoxychloride, Reduction, Strepyomycin
Abstract: A series of novel 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one aliphatic/ aromatic/ heterocyclic amine derivatives were synthesized in good yield. The synthesized compounds were characterized by 1H-NMR, FTIR and elemental analysis. All the synthesized compounds were screened for their in vitro antibacterial activity by agar well diffusion and micro dilution method against standard strains of Gram-Positive (Bacillus Subtilis MTCC 121 and Staphylococcus epidermidis 435), and Gram-negative (Xanthomonas Campestris 7903 and Pseudomonas aeruginosa MTCC 7908) bacteria. Compounds with substituted heterocyclic piperazine moiety showed good activity. In particular, compound 6i showed two fold better activity compared to the standard drug Strepyomycin sulphate.
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Krishnamurthy Byregowda, Vinaya Kambappa, Rakshith Devraj, Shivaramu Prasanna Doddakunche and Subbegowda Rangappa Kanchugarakoppal, Synthesis of 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2- a] pyrimidin-4-one Derivatives as Antibacterial Agents, Medicinal Chemistry 2013; 9 (2) . https://dx.doi.org/10.2174/1573406411309020008
DOI https://dx.doi.org/10.2174/1573406411309020008 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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