Studies on Chemotherapeutics for Mycobacterium tuberculosis. XI

Synthesis and Antibacterial Activity on Mycobacterium tuberculosis of p-Aminosalicyloylhydrazone

Abstract

Twelve kinds of hydrazone were prepared by the application of p-aminosalicylic acid hydrazide to 12 kinds of aldehydes and ketones including orsellinaldehyde, β-orsellinaldehyde, 5-ethyl-2, 4-dihydroxybenzaldehyde, 3-chloro-2, 4-dihydroxy-5-amylbenzaldehyde, methyl isohaemmatomate, and usnic acid. A total of 44 kinds of compounds including these and other known substances were submitted to in vitro tests against tubercle bacilli H₃₇Rv but none had greater activity of inhibiting growth than PAS at 0.156-0.625γ/cc. None of the compounds tested showed any specific antibacterial action against PAS-resistant strains. Growth inhibition was observed with 0.313γ/cc. of p-aminosalicyloylhydrazones of ethyl acetoacetate, salicylideneacetone, and p-dimethyl aminobenzaldehyde, and with 0.63γ/cc. of p-aminosalicyloylhydrazones of ethyl methyl ketone and anisaldehyde.