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Research partially supported by grants from NSERC  相似文献   
88.
An enhanced one-pot synthesis of new functionalized 5,6-dihydro-5,5-dimethyl-2-phenyl-2H-pyridazino[3,4,5-kl]acridin-1(4H)-one derivatives with different substituted patterns by using mesoporous MCM-41 catalyst via a ring opening/ring closure reaction process has been established. This MCM-41 silica catalyst has been synthesized and characterized using an array of sophisticated analytical techniques like BET, XRD, UHRTEM, etc. This reaction could be conducted from inexpensive substrates within short period under neat reflux conditions. Compared with the usual methods, the remarkable advantages of this method are milder reaction conditions, operational simplicity, higher yields, short reaction times and an environmentally friendly procedure.  相似文献   
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Smithia conferta Sm. (Leguminasae), is a commonly used plant in Indian traditional medicine. In the current study anti-ulcer activity of its petroleum ether, alcohol and aqueous extracts of leaves were investigated using different animal models. All extracts were also subjected to phytochemical analysis and their toxic potential. Petroleum ether extract was found to contain steroids; alcohol extract revealed the presence of isoflavonoids, alkaloids and carbohydrates; while aqueous extract was found to contain amino acids, carbohydrates and flavonoids. S. conferta aqueous and alcoholic extracts were found to be non-toxic up to 5000 mg/kg dose level while petroleum ether extract was safe only up to a dose of 2000 mg/kg after single dose administration of the extracts.During confirmation of the claimed anti-ulcer activity, treatment with aqueous and alcoholic extracts showed significant reduction in ulcer index, free acidity as well as total acidity in pylorus ligated rats. However, petroleum ether extract showed relatively less profound reduction in all these indices. The anti-ulcer activity observed in aqueous extract treatment group was nearly equivalent to the standard group.  相似文献   
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The objective of present investigation was to improve the solubility of Eugenol by preparing the inclusion complex of Eugenol with hydroxypropyl-β-cyclodextrin (Hp-β-CD) and characterize the prepared complex by using NMR and differential pulse voltammetry (DPV). Phase solubility curve was plotted using Hp-β-CD in ranging from 0-40 mM of Hp-β-CD and found to be linear. Therefore, inclusion complex was prepared in equimolar ratio of Eugenol and Hp-β-CD by lyophilization method. Fourier transform infrared spectroscopy (FT-IR), (1)H-NMR and DPV were performed for Eugenol, Hp-β-CD and prepared inclusion complex of Eugenol. 2D (two dimensional) NMR was also performed for prepared inclusion complex. The proton of phenol moiety of Eugenol experienced a pronounced chemical shift variation in (1)H-NMR. The positive sign of the variation for proton in (1)H-NMR indicated that the proton was located near to an oxygen atom in the Hp-β-CD cavity and its magnitude showed a strong interaction between -OH proton of Eugenol and Hp-β-CD. 2D NMR confirms the interaction between phenolic group and hydrogen atoms of Hp-β-CD. A well defined anodic peak current corresponding to oxidation of Eugenol in non-encapsulated and Hp-β-CD-Eugenol inclusion complex in phosphate buffer (pH 6.8) was obtained at about 0.35 V and 0.40 V, respectively. The positive shift in oxidation potential indicated the formation of complex via hydrophobic interactions. The oxidant power of Eugenol was retained in complex form as indicated by DPV results. Thus, its oxidation dependent pharmacological property such as antimicrobial activity is not affected after complexation with Hp-β-CD. Thus, (1)H-NMR, 2D-NMR and DPV techniques can be used as valuable tools to determine the mechanism of complexation and state of electrochemical active drug in inclusion complex.  相似文献   
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