Monovalent와 bivalent aminoantipyrine 유도체의 합성과 항염 진통활성

Synthesis and Antiinflammatory-analgesic Activity of Monovalent and Bivalent Aminoantipyines

Six novel 4-aminoantipyrine derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiiflammatory-analgesic activity were compared with antipyrine. Succinyl chloride and Ac20 were reacted with glycine, respectively to give glycine compounds (3-4, 9-10), which were treated with hydroxysuccinimide and dicyclohexyl carbodiimide to yield active esters (5-6,11-12), and then reacted with 4-aminoantipyrine to prepare 4-aminoantipyrine derivatives (7-8, 13-14). 4-Aminoantipyrine reacted with succinyl chloride and Ac20, respectively to give succinyl leis aminoantipyrine (15) and acetyl aminoantipyrine (16). Compounds (7), (8) and (13) gave comparable antiinflammatory activity to antipyrine.