SYNTHESIS CHARACTERIZATION AND PHARMACOLOGICAL EVALUATION OF PYRIMIDINE DERIVATIVES

Abstract

Twenty four compounds were designed by changing the substitution in phenyl ring at fourth position and oxygen and sulphur in the dihydropyrimidone ring All the compounds exhibit the safer result and good bioavailability All the compounds obeyed the Lipinskis five rule and Jorgensens rule of three The docking studies were carried out for those twenty four compounds using glide and molegro software against the cancer tubercular and HIV target All the compounds exhibit good binding energy and with hydrogen bonds Few compounds exhibit more binding energy than the standard compounds All the compounds were synthesized by conventional method Synthesized compounds were first checked for its purity by melting points and Rf values Compounds with good docking score were characterized by IR NMR 13C NMR and Mass spectroscopy ITU V and VTU exhibited MIC at very low concentration for luciferous phage assay method on antitubercular activity In ITU and VTU exhibit cytotoxic activity against the cell line HCT 116 and ITU exhibit growth inhibition factor at very low dose against HCT 116 and A549 Two compounds ITU and VTUwere used for acute toxicity studies using OCED 423 guidelines both were safe at the dose of 2000mgkg of body weight ITU enhanced the level of detoxifying enzyme GST activity with simultaneous decrease in lipid peroxidation levels in the treatment groups when compared to that of the carcinogen control group newline