Synthetic inhibitors of glucocerebroside β-glucosidase
نویسندگان
چکیده
منابع مشابه
Alpha glucosidase inhibitors.
Alpha glucosidase inhibitors (AGIs) are a unique class of anti-diabetic drugs. Derived from bacteria, these oral drugs are enzyme inhibitors which do not have a pancreato -centred mechanism of action. Working to delay carbohydrate absorption in the gastrointestinal tract, they control postprandial hyperglycaemia and provide unquestioned cardiovascular benefit. Specially suited for a traditional...
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A soil microorganism producing αand β-glucosidase inhibitors was identified as Bacillus lentimorbus, based on the fatty acid and morphological analyses, along with biochemical and physiological tests. The α-glucosidase inhibitor was highly produced by this strain in a culture medium containing 0.25% of sodium glutamate and 0.5% of glucose, pH 8.0 at 30C for 2 days. The α-glucosidase inhibitor f...
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The design and synthesis of a small library of pyrrolidine iminocyclitol inhibitors with a structural similarity to 1,4-dideoxy-1,4-imino-D-arabitol (DAB-1) is reported. This library was specifically designed to gain a better insight into the mechanism of inhibition of glycosidases by polyhydroxylated pyrrolidines or iminocyclitols. Pyrrolidine-3,4-diol 15a and pyrrolidine-3,4-diol diacetate 15...
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The conformational analysis of glycosidases affords a route to their specific inhibition through transition-state mimicry. Inspired by the rapid reaction rates of cyclophellitol and cyclophellitol aziridine-both covalent retaining β-glucosidase inhibitors-we postulated that the corresponding carba "cyclopropyl" analogue would be a potent retaining β-glucosidase inhibitor for those enzymes react...
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The α-glucosidase inhibitory activity of an aqueous extract and compounds from the aerial parts of V. corymbosa was demonstrated with yeast and rat small intestinal α-glucosidases. The aqueous extract inhibited yeast α-glucosidase with a half maximal inhibitory concentration (IC50) of 28.6 μg/mL. Bioassay-guided fractionation of the extract led to the isolation of several compounds, including o...
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ژورنال
عنوان ژورنال: Archives of Biochemistry and Biophysics
سال: 1975
ISSN: 0003-9861
DOI: 10.1016/0003-9861(75)90401-4