Synthesis And Biological Activities Evaluation Of 1, 3-thiazolidin-4-one And 1, 3, 5-triazine Derivatives

1,3-Thiazolidin-4-one and 1,3,5-triazine are both types of broad pharmacophores, which derivatives possess diverse biological activities of antivirus, antibacterial, anti-inflammatory, antitumor etc.. Herein, the synthesis and biological activities of these two types derivatives have been widely studied. A series of 2-hydroxymethyl-3-aryl-1,3-thiazolidin-4-one and 2,4, 6-trisubstituted-1,3,5-triazine compounds were synthesized using a microwave-assisted method, and the antifungal, antitumor, glycosidase inhibitory activities were evaluated.1. A series of new 1,3-thiazolidin-4-one compounds were synthesized by the three-component one-pot cyclocondensation of glyoxylic acid ethyl ester, aromatic amines and mercaptoacetic acid using a microwave-assisted method, further reduction by NaBH4 to obtain new 2-hydroxymethyl-3-aryl-1,3-thiazolidin-4-one compounds. The glycosidase (a-amylase, a-andβ-glucosidase) and tumor cell inhibitory activity were evaluated. The results showed that compounds 39c and 39d have a weak inhibitory activities of a-amylase andβ-glucosidase, but all the compounds have noα-glucosidase inhibitory activity, showing a certiain of selectivity. All compounds have no antitumor activity.2. A series of new 2,4,6-trisubstituted-1,3,5-triazine compounds were synthesized using cyanuric chloride,5-(un)substituted 4,6-dimethyl pyrimidinamine, aniline, fatty amine or alcohol as the starting materials. The activities againet Valsa mali Miyabe et Yamada and Hela cell of all the compounds were evaluated, The results showed that compounds 47n, 47o have a notable inhibitory activity against Valsa mali Miyabe et Yamada. Compound 49b has a better anti-tumor activity.