SYNTHESIS, CHARACTERIZATION, AND TUBERCULOSTATIC ACTIVITY OF NOVEL HETEROCYCLIC COMPOUNDS DERIVED FROM DIMETHYL HETEROAROYLCARBONOHYDRAZONODITHIOATES

[摘要]：A series of dimethyl heteroaroylcarbonohydrazonodithioates (1-5) has been synthesized from various heterocyclic carbohydrazides. N'-(Cycloalkyldiamin-2-ylidene)heteroaroylhydrazides (9-20) were obtained by the substitution of dimethyl heteroaroylcarbonohydrazonodithioates with respective diamines in EtOH or dioxane. In water the substitution was followed by cyclization to 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrimidines (21-23). The compounds obtained were tested in vitro towards M tuberculosis standard strain (H(37)Rv) and two "wild" strains, susceptible (Spec. 192) and resistant (Spec. 210). MIC values for all the compounds tested were within 25-100 mu g/mL which indicated their activity lower than reference drugs used (INH, PZA).

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