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Novel series of naphthyl bearing 1,2,3-triazoles (4at) were synthesized and evaluated for their in vitro antiplasmodial activity against pyrimethamine (Pyr)-sensitive and resistant strains of Plasmodium falciparum. The synthesized compounds were assessed for their cytotoxicity employing human embryonic kidney cell line (HEK-293), and none of them was found to be toxic. Among them 4j, 4k, 4l, 4m, 4n, 4t exhibited significant antiplasmodial activity in both strains, of which compounds 4m, 4n and 4t (~3.0-fold) displayed superior activity to Pyr against resistant strain. Pyr and selected compounds (4n, 4p and 4t) that repressed parasite development also inhibited PfDHFR activity of the soluble parasite extract, suggesting that anti-parasitic activity of these compounds is a result of inhibition of the parasite DHFR. In silico studies suggest that activity of these compounds might be enhanced due to π-π stacking.  相似文献   
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Acetone powder preparations of ventral prostates of adult albino rat exhibit an inhibin-like activity.In vitro cultured ventral prostate explants secrete a substance possessing similar activity which appears to be independent of testicular androgens for its elaboration.  相似文献   
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A technique is described for obtaining a Sertoli cell-enriched and a germ cell-enriched fraction from immature rat testes. Sertoli cell-germ cell associations were obtained by incubating washed seminiferous tubule fragments with Collagenase and Pancreatin. They were then manually dissociated into a suspension comprising Sertoli cells as well as the various germ cell types characteristic for a given day of ontogeny. Fractionation into a Sertoli cell-enriched fraction and a germ cell-enriched fraction was effected by centrifugation following layering over a stepwise gradient of Ficoll-400. While the time-span compares favourably with other procedures reported in the literature, it is believed this is the first time a method is described that enables the simultaneous recovery of both the Sertoli cells and the germ cells.  相似文献   
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We studied dependency of toluene oxidation-blended n-decane on blending ratio and temperature using the reactive molecular dynamics (RMD) simulations with the newly developed reactive force field (ReaxFF). Different initial reaction pathways of toluene were observed between pure and blended toluene, while that of n-decane showed little contrast. The differences in toluene oxidation paths are related to radical pool, which is largely influenced by H/C ratio. We analysed the influence of H/C ratio on the consumption of intermediate species, and found different dependencies of HCHO consumption on H/C ratio for different temperatures. The difference is attributed to the large active energy difference between the two main HCHO consumption reactions by OH and O2. For the production part, the OH producing pathway was analysed carefully and shows H/C ratio influences OH production via H production and H abstract reactions. Our RMD simulations show that H/C ratio plays an important role in the oxidation of fuel.  相似文献   
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