STRUCTURE AND ACTIVITY RELATIONSHIP OF MONOAMINE OXIDASE INHIBITORS, PHENYLACETYLHYDRAZIDE DERIVATIVES

[摘要] References(12)Cited-By(2)Since the introduction of iproniazid, originally synthesized as antitubercular drug, monoamine oxidase (MAO) inhibitors have been applied to the treatment of mental depression and angina pectoris. Most of the MAO inhibitors are chemically hydrazine and hydrazide derivatives. It is suggested by many investigators that pharmacological effects of the inhibitors derive from accumulation of serotonin and catecholamines in the central nervous system and other organs. The socalled side effects of the inhibitors such as liver damage are supposed to be due to unknown direct effects. Efforts to find out less toxic inhibitors have been done, thereupon. The present paper describes the structure-activity relationship of new MAO inhibitors, phenylacetylhydrazide derivatives by use of iproniazid and phenylisopropylhydrazine (JB-516) as control. The chemical structures of the derivatives are shown in Fig. 1.

[学科分类] 药理学