The reaction of the N³-substituted amidrazones with dimethyl acethylenedicarboxylate in absolute ethanol at the temperature of -10°C led to the formation of derivatives of dimethyl 2-[(1-aryl-amino-1-arylmethylidene)hydrazono]succinate. Only amidrazone containing two 2-pirydyl substituents gave methyl 2-[5-oxo-3,4-di-(-2-pirydyl)-1,4,5,6-tetrahydro-1,2,4-triazine-6-ylidene)acetate (1) under above-mentioned conditions. Cyclization of other linear products was carried out in methanol solution in the presence of triethylamine [1].

Depending on the type of substituent 5-oxo-1,2,4-triazine derivatives show different fungi- and bacteriostatic activity. The highest activity exhibited compound 1, which inhibited the growth of Staphylococcus aureus, Escherichia coli, Brucella abortus, Mycobacterium smegmatis and Candida albicans in concentration of 125-250 μg/ml. The acute toxcity of this compound in mice was low (>2000 mg/kg i.p.) [1].

Considering to these findings we continuated studies on the antifungal activity of compound 1 using 22 strains of Candida albicans (6 strains resistant to fluconazole and itraconazole) and 7 strains Candida non-albicans (2 strains resistant to fluconazole and itraconazole) isolated from various clinical materials at the University Hospital in Bydgoszcz. Antifungal activity was measured by the disc-diffusion method under standard conditions using Mueeller-Hinton agar medium. The results were read after 24 hours incubation at 35°C. Antifungal activity expressed as minimal inhibitory concentration (MIC) values in μg/ml. It was observed that the growth of only one strain of Candida albicans one strain of Candida non – albicans were inhibited by compound 1 in a relatively low concentration 128 and 256 μg/ml respectively.

References:
[1] Modzelewska-Banachiewicz, B; Kałabun J.; Pharmazie, 54, 7, 503-505 (1999)

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