Search

In a continuing search for new biologically active agents derived from indolizine, 3-(2-aminoethyl)-2-methylindolizine, 3-(2-aminoethyl)-2-methyl-5,6,7,8-tetrahydroindolizine, and some mono- and di-N-substituted derivatives were prepared. Initial pharmacological screening showed that these compounds possess anti-5-hydroxytryptamine, antihistamine, antiacetylcholine, and CNS-depressant activities.

The syntheses and a preliminary pharmacological evaluation of some aminopropylindolizines and aminopropyltetrahydroindolizines are reported. All compounds showed anti-5-hydroxytryptamine, anti-histamine, and antiacetylcholine activities. Some also exhibited weak CNS activity.

Synthesis and study of the antimonoamine oxidase activity of some N'-substituted hydrazides of 2-methyl-3-indolizinecarboxylic acid are reported. The activities were generally of about the same order as those of the corresponding hydrazides of 2-indolizinecarboxylic acid.

The synthesis and antimonoamine oxidase activity of some N'-substituted hydrazides of indolizine-2-carboxylic acid are described. They all inhibit monoamine oxidase and are more active than iproniazid. The structure-activity relationships also are discussed.