Synthesis of new derivatives of pyrimido[5,4-e][1,2,4]triazolo[3,4-b][1,3,4]thiadiazine and stadise of their biological activities

Abstract

Due to their unique clinical applications, syntheses of pyrimidine-fused heterocycles have been intensively investigated in recent years. Pyrimidine derivatives are highly effective as hypnotic drugs, antitumor, antibacterial and anti-HIV agents, and in cancer detection [1-3].Moreover the pyrimido[4,5-e][1,3,4]thiadiazines are a class of heterocyclic compounds, which have been described as anti-hypertensives [4], with enzyme inhibitory activity on soybean 15-lipoxygenase [5]. We now describe the synthesis of some new derivatives of tricyclic pyrimido[5,4-e][1,2,4]triazolo[3,4b][1,3,4]thiadiazines and their enzyme inhibitory activity towards 15-LO (Scheme 1).