Cardiac-slowing amidines containing the 3-thioindole group. Potential antianginal agents

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Abstract
A series of 3-thioindolamidines (and 3-indolamidines) related to mixidine (1) was studied for cardiac-slowing properties in dogs, following the discovery of activity for prototype thioindole. Structure-activity relationships were explored, leading to many potent antitachycardiac agents [e.g., N''-[2-(indol-3-ylthio)ethyl]-N,N-dimethylethanimidamide (45)]. Cardiac-slowing activity is enhanced by substitution of the indole nitrogen with small (C1-C3) saturated alkyl groups, unsaturated alkyl groups or a methoxyethyl group; replacement of the N-methyl group with alkyl or phenyl groups; and extension of the ethylene bridge by 2 methylene units. Dethio (i.e., 3-indole) analogs of prototype thioindole with alkyl substitution of the indole nitrogen have greater activity as well. Several potent compounds were less also found to have minimal myocardial depression, e.g., (45).

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