Anti-inflammatory, analgesic properties and antipyretic action of 2-amino-1,2,3,4-tetrahydroisoquinoline-1,3-dione and its derivatives

Abstract

The analgesic and sedative effects of tetrahydropalmatine, tetrahydroberine and tetrahydroisoquinoline derivatives have been recognized. In order to discover new derivatives of tetrahydroisoquinoline with pharmacological properties similar to tetrahydropalmatine and with a simpler, easily synthesizable structure, several new derivatives of tetrahydroisoquinoline were synthesized. They were examined for their anti-inflammatory effect and analgesic effect in mice using Whittle's method and for their antipyretic effect in rats with endotoxin. 2-Amino-1, 2, 3, 4-tetrahydroisoquinoline-1, 3-dione was found to possess equally effective anti-inflammatory and analgesic properties as the reference drug, aminopyrine. It was found that this compound at 25 mg/kg, p. o. was as effective in its antipyretic action as aminopyrine at 100 mg/kg, p. o. Among other 13 new derivatives, 2-dimethylaminoethyl-1, 2, 3, 4-tetrahydroisoquinoline-1, 3-dione was also found to possess a similar degrees of anti-inflammatory and analgesic effect as aminopyrine.