CHEMOTHERAPY OF EXPERIMENTAL TUBERCULOSIS .6. DERIVATIVES OF ISONIAZID

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Abstract
A series of derivatives of isoniazid were prepared and tested in vitro and in vivo against Mycobacterium tuberculosis. Some generalizations concerning the relation of structure to antituberculous activity were made. Introduction of a substituent in the pyridine ring results in loss of in vitro and in vivo activity. The reduction of the pyridine ring causes loss of activity. Alkylation or acylation of the hydrazine N produces derivatives which are active in vivo although they have low in vitro activity. Condensation of isoniazid with aldehydes and ketones yields derivatives which are active both in vitro and in vivo. None of the compounds tested is more active on a molar basis than isoniazid.