Medicinal Chemistry

Author(s): Byregowda Krishnamurthy, Kambappa Vinaya, Devraj Rakshith, Doddakunche Shivaramu Prasanna and Kanchugarakoppal Subbegowda Rangappa

DOI: 10.2174/1573406411309020008

Synthesis of 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2- a] pyrimidin-4-one Derivatives as Antibacterial Agents

Page: [240 - 248] Pages: 9

  • * (Excluding Mailing and Handling)

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