Synthesis of 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido1,2-a pyrimidin-4-one derivatives as antibacterial agents

Krishnamurthy, B. and Vinaya, K. and Rakshith, D. and Prasanna, D. S. and Rangappa, K. S. (2013) Synthesis of 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido1,2-a pyrimidin-4-one derivatives as antibacterial agents. Medicinal Chemistry, 9 (2). pp. 240-248. ISSN 1573-4064

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Official URL: http://doi.org/10.2174/1573406411309020008

Abstract

A series of novel 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H- pyrido1,2-apyrimidin-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.

Item Type: Article
Uncontrolled Keywords: 2 a]pyrimidin 4 one, 2 methyl 3 2 (thiazol 2 ylamino)ethyl 6, 2 methyl 3 2 (tetrahydrofuran 2 yl)methylamino]ethyl] 6, 2 methyl 3 2 2 methyl 1H imidazol 1 yl)ethyl]2 methyl 6, 3 (2 chloroethyl) 2 methyl 4H pyrido 1, 3 (2 chloroethyl) 2 methyl 6, 3 1 (pyridin 2 ylamino)ethylidene] dihydrofuran 2(3h)one, 3 2 (4 fluorobenzylamino)ethyl 2 methyl 6, 3 2 (6 ethoxybenzod]thiazol 2 yl amino)ethyl] 6, 3 2 (cyclopentylamino)ethyl 2 methyl 6, 3 2 (furan 2 ylmethylamino)ethyl 2 methyl 6, 3 2 (hexylamino)ethyl2 methyl 6, 3 2 (4 aminophenyl)(phenyl)amino]ethyl]2 methyl 6, 3 2 1 (3, 3 2 4 (2 aminoethyl)piperazin 1 yl]ethyl] 2 methyl 6, 3 2 4 (2 aminoethyl)piperazin-1 yl]ethyl] 2 methyl 6, 3 2 4 (2 fluorophenyl)piperazin 1 yl]ethyl] 2 methyl 6, 3 2 4 (hydroxydiphenylmethyl) piperidin 1 yl]ethyl] 2 methyl 6, 3 2 4(5 fluorobenzodisoxazol 3 yl)piperidin 1 ylethyl 2 methyl 6, 3 2 benzyl(methyl)aminoethyl 2 methyl 6, 4 diethoxybenzyl) 5, 6 diethoxyisoindolin 2 yl)ethyl2 methyl 6, 7, 8, 9 tetrahydro 4H pyrido1, agar diffusion, Amines, Anti-Bacterial Agents, antibacterial activity, antiinfective agent, article, Bacillus subtilis, Bacteria, broth dilution, Chemistry Techniques, drug synthesis, Fourier transform infrared photoacoustic spectroscopy, Gram negative bacterium, Gram positive bacterium, heterocyclic compound, human, in vitro study, Microbial Sensitivity Tests, nonhuman, piperazine, priority journal, proton nuclear magnetic resonance, Pyrimidinones, standard, Staphylococcus epidermidis, streptomycin sulfate, Synthetic, unclassified drug, Xanthomonas campestris
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 15 Oct 2019 05:17
Last Modified: 15 Oct 2019 05:17
URI: http://eprints.uni-mysore.ac.in/id/eprint/8977

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