A series of triazoloquinazolines and triazinoquinazolines were synthesized as novel anti-inflammatory agents. Some of the newly synthesized compounds 8, 11, and 19 showed good anti-inflammatory activities. Also, the median lethal doses (LD_50s) of compounds 8, 11, and 19 in mice were 222.25, 213.25, and 235 mg/100 g b.w., respectively. Oral administration of compounds 8, 11, and 19 to the rats at dose of 300 mg/kg b.w. for 10 days showed non-significant changes in liver enzymes SGOT, SGPT, ALP, LDH, γ-GT, SOD, GPx, and blood GSH and serum TBARs as compared with the control group. But, administration of indomethacin orally to the rats at a concentration of 600 mg/kg b.w. daily for 10 days to rats showed significant increase in serum SGOT, SGPT, ALP, LDH, γ-GT, and TBARs and significant decrease in blood GSH, SOD, and GPx. These findings suggest that compounds 8, 11, and 19 exhibited good anti-inflammatory activity and more safe on liver enzymes in rats.