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Synthesis and Characterization of Some Novel 2-(Trifluoromethyl)pyrimido[1,2-<b><i>a</i></b>]benzimidazoles and Pyrimido[1,2-<b><i>a</i></b>]benzimidazol-2<b><i>H</i></b>)-ones of Biological Interest
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2006
Year
Medicinal ChemistryDerivativesBioorganic ChemistryBiochemistryBiological InterestSignificant Dna-topoisomeraseNatural SciencesMedicineFluorous SynthesisMethyl KetonesOrganic Chemistry2D-nmr ExperimentsHeterocycle ChemistryChemical BiologyPharmacologyPharmaceutical ChemistryDrug Discovery
The synthesis of some potentially active 2-(trifluoromethyl)pyrimido[1,2-a]benzimidazoles and pyrimido[1,2-a]benzimidazol-2(1H)-ones by the cyclization of 4-alkoxyvinyl trifluoro(chloro)methyl ketones with 2-aminobenzimidazole is described. The structure of the products was assigned based on 1H and 13C NMR as well as 2D-NMR experiments. Some of the obtained products exhibited significant DNA-topoisomerase I inhibitory activity.