THE CHEMOTHERAPY OF EXPERIMENTAL TUBERCULOSIS I

Abstract

The in vitro activities against the BCG strain of Mycobacterium tuberculosis of a number of thiosemicarbazones and related compounds were detd., and from these activities certain general correlations as to structure and in vitro activity are made. Thiosemicarbazide and its alkyl derivatives are active in vitro, but its acyl derivatives are, in general, inactive. Thiosemicarbazones formed from aliphatic carbonyl compounds are inactive. Condensation of aromatic aldehydes or cinnamic aldehydes with thiosemicarbazide will give active derivatives, but condensation with 3- and 4-substituted thiosemicarbazides will give inactive derivatives. No apparent correlation exists between the substituents in aromatic aldehydes and the activity of their corresponding thiosemicarbazones. Thiosemicarbazones derived from aromatic ketones are active in vitro although somewhat less active than the thiosemicarbazone from the corresponding aldehyde. Thiosemicarbazones derived from heterocyclic aldehydes will also be active although somewhat less active than benzaldehyde thiosemicarbazone.