Sg. Kucukguzel et al., Synthesis, characterization and pharmacological properties of some 4-arylhydrazono-2-pyrazoline-5-one derivatives obtained from heterocyclic amines, EUR J MED C, 35(7-8), 2000, pp. 761-771
The synthesis of a new series of 4-arylhydrazono-2-pyrazoline-5-ones 7-24 a
nd 22a is described. Structures of the synthesized compounds were confirmed
using UV, IR, H-1-NMR, C-13-NMR and EI-mass spectral data. These compounds
were tested in vitro against one Gram-positive and two Gram-negative bacte
rial strains, two mycobacterial strains and a fungus, Candida albicans. Com
pound 22 was found to be more active against Staphylococcus aureus than the
other compounds at a concentration of 15.6 mu g/mL. Some related compounds
were evaluated for anticonvulsant activity. Compound 11 showed 40% protect
ion against pentylenetetrazole-induced seizures in albino Swiss mice. In vi
tro antituberculosis activity of 4-arylhydrazono-2-pyrazoline-5-ones 7-12,
14-24, 22a and coupling products 6a-f were tested on Mycobacterium tubercul
osis H37Rv. Of these compounds, only 24, which exhibited > 90% inhibition i
n the primary screen at 12.5 mu g/mL against this strain was re-examined fo
r determination of its actual MIC. However, level II assay revealed that th
e MIC value was not less than 12.5 mu g/mL. The same compound was also test
ed against Mycobacterium avium, which was observed not to be susceptible to
24. (C) 2000 Editions scientifiques et medicales Elsevier SAS.