Effect of zearalenone on the activity of some steroid transforming enzymes in rats

Zearalenone, a mycotoxin with estrogenic activity, is used in vivo to study its effect on some steroid transforming enzymes. The enzyme activities of 5 beta-reductase [EC. 1.1.1.125] and 17 beta-hydroxysteroid dehydrogenase [EC. 1.1.1.25] are involved in the metabolism of progesterone and estradiol-17 beta-. These hormones are responsible for the formation of mature ovum and prevention of abortion in females. Zearalenone was injected subcutaneously at a dose of 3.3 mg/kg body weight to female mature rats at estrus phase. Control rats were injected with 0.5 ml corn oil. After 48 hours treatment time, liver, uterine tissues and serum samples were used for enzymes assay using spectrophotometric methods. The activity of 5 beta reductase from hepatic and uterine preparations and serum samples was significantly higher in Zearalenone treated rats than that of control group [p < 0.0001]. The results also showed a significant increase in the activity of 17 beta-hydroxysteroid dehydrogenase [17beta-HSD] in the samples obtained from Zearalenone treated rats as compared with that of the control group [P < 0.0001]. Furthermore, the estrogenic effect of Zearalenone on the uterine weights of female rats was noted

Synthesis of certain thienopyrimidone derivatives as possible anticonvulsants

Several thienopyrimidone derivatives were synthesized and evaluated for their anticonvulsant activity. This was achieved via reacting 2- hydrazinocarbonylmethylthio-3-pheny1-3, 4, 5, 6, 7, 8-hexahydrobenzo [4, 5] thieno[2, 3-d] pyrimidine-4-one [Ib] with carbon disulphide in ethanolic potassium hydroxide to give the respective oxadiazole [III]. Application of the Mannich reaction to the intermediate [III], using formaldehyde and different secondary amines yielded the corresponding Mannich bases [IV]. Condensation of either 2-mercapto-3-phenyl-3, 4, 5, 6, 7, 8-hexahydrobenzo [4, 5] thieno [2, 3-d] pyrimidin-4-one [I] or the substrate [III] with a variety of alkyl halides or N- substituted chloroacetamide afforded the corresponding thioether's [II and V] respectively. The pharmacological screening has revealed that two of the novel compounds show slight anticonvulsant activity

Synthesis and mass spectral studies of some 1- [2-benzimidazolyl] or [6-methyl-4 [1H] -pyrimidinon-2-yl] -5-substituted phenyl-3-methylpyrazoles

New 1-[2-benzimidazolyl] 5-substituted phenyl-3- methylpyrazoles [IV] and 1-[6-methyl-4 [1H] -pyrimidinon-2-yl]-5-substituted phenyl-3- methylpyrazoles [V] have been synthesized by the condensation of beta- diketones [III] and 2-hydrazinobenzimidazole [I] or 2-hydrazino-6- methyluracil [II], respectively. Bromination study of IV and V in Br2/ACOH has revealed that electrophilic attack of bromine occurs in pyrazole ring at position 4 and in uracil ring at position 5. The general spectral fragmentation mode of these compounds has been studied