A short and flexible route to aza-beta-(1 -> 6)-C-disaccharides: Selective alpha-glycosidase inhibitors
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The reaction of an aldehyde, an isocyanide, N-methylhydroxylamine, and acetic acid in the presence of 4-.ANG. mol. sieves afforded alpha -keto amides in moderate to good yields. In contrast, 3-.ANG. mol. sieves did not promote the desired multicomponent re ...
A 33-residue de novo designed peptide ligase is reported which catalyzes the template-directed condensation of suitably activated short peptides with catalytic efficiencies in excess of 105 ([kcat/Km]/kuncat). The ligase peptide, derived from natural and d ...
3,6-Anhydro-1-(aryl or alkylamino)-1-deoxy-D-sorbitol derivatives have been prepared in four steps from isosorbide, a by-product from the starch industry. The inhibitory activities of these new compounds have been evaluated towards 13 glycosidases. A first ...
Combinatorial mutagenesis was used to investigate the role of three key residues in cytochrome c peroxidase (CCP) from Saccharomyces cerevisiae, Arg48, Trp51, and Trp191, in control of the reactivity and selectivity of the heme-contg. enzyme. Libraries wer ...
2002
Structure and dynamics of substrate binding (cefotaxime) to the catalytic pocket of the mononuclear zinc-beta-lactamase from Bacillus cereus are investigated by molecular dynamics simulations. The calculations, which are based on the hydrogen-bond pattern ...
Oxidn.-sensitive nanoparticles have been decorated with an oxidizing enzyme (glucose oxidase) for release behavior that is responsive to the presence of the enzyme substrate (glucose). [on SciFinder (R)] ...
The Diels-Alder adduct of 2,4-dimethylfuran to 1-cyanovinyl (1'R)-camphanate ((+)-(1R,2S,4R)-2-exo-cyano-1,5-dimethyl-7-oxabicyclo[2.2.1]hept-5-en-2- endo-yl (1'R)-camphanate ((+)-1)) was converted into (+)-2,7-dideoxy-2,4-di-C-methyl-L-glycero-((+)-6) and ...
The activity of penicillin acylase has been studied in aq. and org. solvents, as free enzyme as well as immobilized within the membrane of liq.-core capsules. The activity of the enzyme is inhibited by the accumulation of the products of the hydrolysis rea ...
2005
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This paper describes the preparation, characterization, and enzymatic activity of complex coacervate core micelles (C3Ms) composed of poly (acrylic acid) (PAA) and poly (N- methyl-2- vinyl pyridinium iodide)-b-poly (ethylene oxide) (PQ2VP-PEO) to which the ...
2007
The conversion of 2,2-difluoro-1,3-benzodioxole, an exceptionally acidic arene, via a 4-lithiated intermediate into more than three dozen new derivs. was conceived as a case study. The lithiated species was trapped by C0-electrophiles (4-toluenesulfonyl az ...