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Studies on the Combination of Drugs. VI. : Effect of 4-Hydroxyantipyrine Etheral Derivatives on Metabolism of Aminopyrine, Phenacetin, Acetanilide, and Phenylbutazone

1968; Pharmaceutical Society of Japan; Volume: 88; Issue: 7 Linguagem: Inglês

10.1248/yakushi1947.88.7_847

1347-5231

Taiji Nakayama,

Synthesis and Reactions of Organic Compounds

By the joint use of 4-hydroxyantipyrine (HOAT), being the metabolites of aminopyrine and antipyrine, some of the metabolism in pyrazolone, aniline, pyrazolidione and barbitar series of medicinals, was found to be suppressed. In order to prepare more effectelongating substances than HOAT, ether derivatives of the hydroxyl group of HOAT in 4 position were synthesized, and their influence on the metabolism of aminopyrine, phenacetin, acetanilide and phenylbutazone was examined by comparing with the SKF 525-A which is an enzyme inhibitor in the metabolism of medicinals. However no suppressive action of ether derivatives on the metabolism of medicinals were observed, and any synthetic treatment of HOAT in OH group is not found to be effective. As to SKF 525-A and HOAT, the former showed a stronger action in the suppression of aminopyrine metabolism, but to the inhibitory action of metabolism of phenacetin, acetanilide and phenylbutazone, both showed nearly the same action.