Studies on the Antituberculous Activity of the Derivatives of Cinnamic Acid Hydrazide

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Recently, a new antituberculous antibiotic was isolated by Ohkuma et al. and named as Tuberin. The chemical structure of Tuberin was then indenti fied as trans-p-methoxystyrylamine and it was synthesized from trans-p-methoxycinnamic acid by Anzai. In the course of this chemical research, some derivatives of cinnamic acid hydrazide were prepared as the intermediate compounds to Tuberin synthesis by him. The present authors had an op portunity to examine those compounds in vitro and in vivo for antituberculous activity. The minimum inhibitroy concentrations against H37Rv and its iso-niazid-resistant variant strain (H37RvINH-R) ini Kirchner semisolid agar medium are as shown in, Table 1, namely they are ranging from 4 to 32mcg/ml against H37Rv. Of particular interest is the fact that H37RvINH-R is more or less resistant to those derivatives of cinnamic acid hydrazide. The antituber culous activity against experimental mouse tuber culosis of the derivatives was examined two times, in the designs as shown in Table 2 and 3, and the results are presented in Fig. 1 and 2. It will be seen from these figures that the test samples have chronic toxicity and are not effective against intrave nous infection of mice. The compounds would not: have practical value.
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