A small set of nojirimycin- and pyrrolidine-based iminosugar derivatives has been synthesized and evaluated as potential inhibitors of porcine and insect trehalases. Compounds 12, 13 and 20 proved to be active against both insect and porcine trehalases with selectivity towards the insect glycosidase, while compounds 10, 14 and 16 behaved as inhibitors only of insect trehalase. Despite the fact ...

In addition to physical problems, acne caused by Staphylococcus aureus frequently leads psychological problems as well. As a result, Treatment therapy using antibiotics in the long term and at inappropriate doses increases rate of antibiotic resistance. Alternative treatments can be performed natural ingredients, such cherry leaves ( Muntingia calabura ), which exhibit antibacterial properties....

A qualitative and qwantitative study of the glycosidnl content of the different organs and parts of Citrullus colocynthis SCHRAD. were undertaken. Qualitative study revealed the presence af a-elateri~r 2-D-glucopyranoside and its aglycone in all organs; cucurbitacin B, I , and'L (both free and glycosidal forms) in stents, leaves, and fruits. A suggested procedure for the estimation of a-elateri...

to its glycoside (arachidoside) content. On the basis of in creased excretion of phenols in the group of rats fed arachi doside, and of an increased iodine content in the phenolic fraction of the urine as compared with the control, it was sug gested that this glycoside acted as an antithyroid compound by forming molecular compounds with elemental iodine in the gland. Confirmatory evidence for t...

Fermentation of Dactylosporangium sp. (ATCC 53693) produces a mixture of tetracycline derivatives from which several related tetracycline glycosides, the dactylocyclines, were isolated and their structures determined. The most abundant glycoside in initial fermentations was found to be dactylocycline A. Each glycoside proved to be acid sensitive and readily hydrolyzed to a common aglycone, dact...

The purpose of this study was to see whether the receptor for cardiac glycosides might be localized upon or within the plasma membrane of digitalis-sensitive cells. Ouabain and digoxin were joined covalently to several large protein molecules. These macromolecular conjugates are too large to enter intact cells; consequently, any pharmacologic or biochemical effects which they display should ari...

Using structural insight, the binding mode of isofagomine-derived inhibitors with family GH9 glycosidases is achieved via the study of Alicyclobacillus acidocaldarius (AaCel9A) endoglucanase. In contrast to what was observed in the first report using these compounds with inverting glycosidases from family GH6, these inhibitors do not adopt a distorted conformation in the active site.

Competitive glycosidase inhibitors are generally sugar mimics that are costly and tedious to obtain because they require challenging and elongated chemical synthesis, which must be stereo- and regiocontrolled. Here, we show that readily accessible achiral (E)-1-phenyl-3-(4-strylphenyl)ureas are potent competitive α-glucosidase inhibitors. A systematic synthesis study shows that the 1-phenyl moi...