Mefentrifluconazole, a novel azole derivative, serves as a broad-spectrum antifungal agent in agrochemical applications. It acts as a potent, selective, and orally active inhibitor of fungal CYP51 (Kd=0.5 nM), while exhibiting reduced inhibitory activity against human aromatase (IC50=0.92 μM) [1].
体内研究
Mefentrifluconazole undergoes comprehensive toxicity assessments, including full reproductive toxicity studies. Long-term repeated dose toxicity and/or carcinogenicity investigations have been carried out in rats, mice, and dogs. In each species, the highest tested dose level induces systemic toxicity [1].
In acute and repeat dose toxicity studies conducted with Mefentrifluconazole, single-dose administration to rats yielded LD50 values of >2000 mg/kg bwt orally, >5000 mg/kg bwt dermally, and >5.314 mg/L by inhalation as a dust aerosol. Mefentrifluconazole does not induce skin or eye irritation, nor does it exhibit phototoxicity in vitro[1].
In the acute neurotoxicity study in rats, Mefentrifluconazole (administered orally at 2000 mg/kg bwt as a single dose) resulted in decreased body weight gain and transient neurobehavioral effects observed only on the day of treatment, including unsteady gait, reduced motor activity, decreased grip strength of the forelimbs, and increased distance between the hind limbs in the landing foot-splay test [1].
In the repeated-dose toxicity studies, the liver was identified as the target organ across all three species examined. Higher dose levels in rats (oral diets; 383/334 mg/kg/bwt/d (4000 ppm)) and C57BL/6JRj mice (61 mg/kg bwt/d (300 ppm)) resulted in reduced body weight gain and food consumption, altered clinical chemistry parameters, increased liver weight, and exhibited liver cell hypertrophy and/or necrosis. At lower doses, increased liver weight occurred without associated histopathological alterations, indicating an adaptive response to treatment [1].
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