Studies On Synthesis And Biological Activities Of Thieno Pyrimidine Derivatives

Thieno pyrimidine derivatives have wide application prospect in the field of medicine and agricultural chemical due to their good biological and pharmacological activities, Some compounds with thieno pyrimidine moiety have been developed to herbicides, pesticides, fungicides and medicine. In this thesis, we designed and synthesized thieno pyrimidine derivatives which have not been reported in the literature via aza-Wittig reaction. This reaction had the advantages of easily available materials, mild reaction condition and high yield. The necessary conditions for the intermediate to form a ring to get target compounds were explored. Biological activities of the compounds were further studied. The result showed that some of the compounds had good bactericidal activities.Research content of this paper is divided into the following aspects1. 13 kind of 3-phenyl substituted thieno[2,3-d:5,4-d] dipyrimidine-4,5-(3H,6H) diones were synthesized via aza-Wittig reaction. All the compounds were charac-terized by IR, 1H NMR and LCMS.2. 11 kind of 3-(4-methylphenyl) substituted thieno[2,3-d:5,4-d] dipyrimidine-4, 5-(3H,6H) diones were synthesized via aza-Wittig reaction. All the compounds were characterized by IR, 1H NMR and LCMS.3. The synthesized of 24 compounds was divided into five concentration gradient to test the antibacterial activity of tea raw gibberella,rose raw alternaria,tea raw anthracin,tea raw phoma. Most compounds exhibit antibacterial activity, the compound 8d at 100 mg/L concentration inhibitory activity of tea raw gibberella,rose raw alternaria,tea raw phoma were 72%、71%、71%,the compound 8i at 100 mg/L and 200 mg/L concentration inhibitory activity of rose raw alternaria were 74%、82%,the compound 14 b at 100 mg/L concentration inhibitory activity of tea raw gibberella,tea raw anthracin were 80%、81%,the compound 14 e at 100 mg/L concentration inhibitory activity of tea raw gibberella,rose raw alternaria,tea raw phoma were 89%、70%、83%.4. Some of the synthesized compounds were selected to test the stability activities to the of G-quadruplexes, among which, ligand 2(compound 8d), ligand 4(Compound 8j), ligand 5(Compound 8k) exhibited some stabilizing effect to the G-quadruplexes which was formed by ckit1-1DNA chain sequences,The melting temperature was 70.73 ℃, 74.95 ℃, 69.03 ℃higher than the control group,the effect of other ligands is not obvious.