Synthesis and Biological Activities Evaluation of 1, 3-Thiazolidin-4-one and 1, 3, 5-Triazine Derivatives
|Keywords||Thiazolidine-4 - one 1,3,5 - triazine Antibacterial Antitumor Glycosidase inhibitory activity|
1,3 - thiazol -4 - one and 1,3,5 - triazine are broad-spectrum efficacy group , exhibit good physiological activity in the antiviral, antibacterial , anti-inflammatory , anti - tumor, etc. , so synthesis and biological activity of these two types of compounds by the extensive attention . This article using microwave promoted synthesized a series of novel 2 - (hydroxymethyl) -3 - aryl - 1 ,3 - thiazolidine-4 - one and 2,4,6 - substituted 1,3,5 - triazines anti-fungal compounds , and compounds , and preliminary evaluation of anti-tumor and glycosidase inhibitory activity . 1 under microwave conditions with ethyl glyoxylate , aromatic amines , and thioglycolic acid as a starting material , the use of microwave promote the multi-component one-pot synthesis of a series of new 1,3 - thiazolidine-4 - keto compound , NaBH4 further reduced to give 2 - (hydroxymethyl) -3 - aryl -1 ,3 - thiazolidine-4 - keto compound , and test compounds of glycosidases ( α - amylase , α - and β- glucosidase enzyme) and cervical the inhibitory activity of cancer cells . The results indicate that compound 39c and 39d on the α-amylase and β-glucosidase enzymes have a weak inhibitory activity, but all the compounds is not an α - glucosidase inhibitory activity, exhibit a certain selectivity ; Compound 39 did not show anti-tumor activity. 2 with cyanuric chloride as a starting material , 5 - substituted ( non - substituted) -4,6 - dimethyl-2 - amino - pyrimidine, aniline and fatty amine or alcohol synthesized a series of novel 2,4,6 - trisubstituted -1, 3,5 - triazine compounds , and preliminary testing of all compounds active against apple rot bacteria and toxic effects of cervical cancer cells . The results show that the compound 47n , 47o of Cytospora bacteria has significant inhibitory effect : 49b on cervical cancer cell proliferation has better inhibition .