SYNTHESIS, CHARACTERIZATION AND PHARMACOLOGICAL ACTIVITIES OF PYRIMIDINE DERIVATIVES CONTAINING 2-PYRAZOLIN-5-ONE

A new series of thiazolo [3',2';1,2] pyrimido [5,4,e] pyrimidines and thiazolo [3', 2'; 1,2] [1,2,4] triazolo [3'', 4''-c] pyrimido [5,4-e] pyrimidines linked to 2-pyrazolin-5-one moiety were prepared by derivatization of the hydrazine functionality of the heterocyclic hydrazine with various reagents. The newly synthesized compounds were characterized by elemental analyses and spectroscopic techniques. The antimicrobial, anti-inflammatory, and analgesic activities of the synthesized compounds were evaluated using agar diffusion method, carrageenan-induced paw edema, and writhing assays, respectively. The finding of the study showed that, compounds 1a, b, 3a, b, 7b and 15a, b have excellent antimicrobial potency. In the anti-inflammatory activity, compounds 2a and 2b showed remarkable activities (30% and 32%, respectively). For the analgesic activity, the same compounds 2a and 2b gave significant activities (27% and 29%, respectively).