Synthesis of 1,2,3,4-tetrahydro-.BETA.-carboline derivatives as hepatoprotective agents. III. Introduction of substituents onto methyl 1,2,3,4-tetrahydro-.BETA.-carboline-2-carbodithioate.

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Abstract
Dithiocarbamates of various substituted tetrahydro-.beta.-carbolines were synthesized and tested for hepatoprotective activity against carbon tetrachloride (CCl4)-induced liver damage in mice. Structure-activity relationships were investigated. Some neighboring group participation of the 3-substituent with the dithiocarbamate group appeared to be important for the manifestation of activity. The compounds (1a, 2a, and 3i) with hydrophilic substituents at the 3 position exhibited significant activity. Substitution at the 9 position of the 3-carboxylic acid (1a) lowered the activity.