Terinek, Miroslav; Vasella, Andrea published the artcile< Synthesis of tetrahydro-pyrido-imidazole-2-acetates: Effect of carboxy and methoxycarbonyl groups at C(2) on the inhibition of some 尾- and 伪-glycosidases>, Recommanded Product: Methyl 4,4-dimethoxy-3-oxobutanoate, the main research area is hydropyridoimidazoleacetate monosaccharide hydrophobic effect preparation structure property inhibition glycosidase.
The gluco- and manno-tetrahydro-pyrido-imidazole-2-acetates and -acetic acids, e.g. I, were synthesized by condensation, in the presence of HgCl2, of the known thiono-lactam II with the 尾-amino ester III that was obtained by addition of AcOMe to the imine, followed by debenzylation. Title imidazoles were tested as inhibitors of the 尾-glucosidase from Caldocellum saccharolyticum, the 伪-glucosidase from brewer’s yeast, the 尾-mannosidase from snail, and the 伪-mannosidase from Jack beans. There is a similar dependence of the Ki values on the nature of the C(2)-substituent in the gluco- and manno-series. Manno-imidazoles are in general weaker inhibitors than the gluco-analogs. The Me acetates are 3-4 times weaker than the Me propionates, in agreement with the hydrophobic effect. Structure activity of title compounds as inhibitors of glycosidases is reported. The Me propionates proved the strongest inhibitors of the 伪-glucosidase (IC50(5) = 25 渭M) and the 伪-mannosidase (Ki(11) = 0.60 渭M).
Helvetica Chimica Acta published new progress about Condensation reaction. 60705-25-1 belongs to class esters-buliding-blocks, and the molecular formula is C7H12O5, Recommanded Product: Methyl 4,4-dimethoxy-3-oxobutanoate.
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