Itraconazole (ITZ) is a potent inhibitor of CYP3A in vivo. However, unbound plasma concentrations of ITZ are much lower than its reported in vitro Ki, and no clinically significant interactions would be expected based on a reversible mechanism of inhibition. The purpose of this study was to evaluate the reasons for the in vitro-in vivo discrepancy. The metabolism of ITZ by CYP3A4 was studied. T...

Several α-alkylated β-amino esters have been obtained via DKR processes employing a kit of transaminases and isopropylamine as an amino donor in aqueous medium under mild conditions. Thus, while acyclic α-alkyl-β-keto esters afforded excellent conversions and enantioselectivities, although usually low diastereoselectivities, using more constrained cyclic β-keto esters high to excellent inductio...

2,3-Unsaturated-4-keto glycosyl acetates were found to exhibit low reactivity under several glycosylation conditions. Chemoselective glycosylations were effectively performed using 2,3-unsaturated glycosyl and 2,3-dideoxy glycosyl acetates as armed glycosyl donors, and 2,3-unsaturated-4-keto glycosyl acetates as disarmed glycosyl donors.

[reaction: see text] The catalytic enantioselective electrophilic fluorination promoted by quaternary ammonium salt from cinchonine as a phase-transfer catalyst is described. Treatment of beta-keto esters with N-fluorobenzenesulfonimide as the fluorine source under mild reaction conditions afforded the corresponding alpha-fluoro beta-keto esters in exellent yields with good to moderate enantiom...

CMAH CMPN -acetylneuraminic acid hydroxylase CMP-Kdn Cytidine monophospho-2-keto-3 deoxynonulosonic acid CMP-Neu5Ac Cytidine monophosphoN -acetylneuraminic acid CMP-Neu5Gc Cytidine monophosphoN -glycolylneuraminic acid Gal Galactose GlcNAc N -Acetylglucosamine ITIM Immunoreceptor tyrosine-based inhibitory motif Kdn 2-Keto-3 deoxynonulosonic acid Neu5Ac N -Acetylneuraminic acid Neu5Gc N -Glycoly...

A mild, practical and efficient palladium-catalyzed decarboxylative ortho-acylation of O-methyl ketoximes with α-keto acids via C-H bond activation is described. In these reactions, a broad range of O-methyl ketoximes and α-keto acids undergoes the decarboxylative cross-coupling reactions with high selectivities and good tolerance.

Single walled nanotubes (SWNT) are common interested nanovehicle to make biosensors more sensitive.Carbon nanotubes (CNTs) have many distinct properties make them to be exploited to develop the nextgeneration of such nano sensors .The Keto-Enol tautomerization is one of the most common investigatedsubjects of isomerism in this regards, sensors are devices that are able to detect and change the ...

Glycylasparagine has been found to be more effective than aspartic acid in reversing the inhibition of adaptive enzyme synthesis by cysteic acid or P-hydroxyaspartic acid or combinations of these synergistic inhibitors (1). The results were interpreted to indicate a pathway of utilization of the peptide not involving the inhibited enzymatic utilization of the free amino acid. Also, histidine pe...

Previous studies have indicated marked differences in the quantitative distribution of a number of enzymes, as well as other substances, in various histologically distinct areas of the nervous system (l-4). An earlier method (2) for MDH, LDH, and GDH’ in brain required 0.3, 1.5, and 10 y of brain, dry weight, respectively, for the determination of these enzymatic activities. Some of the histolo...

Although the probability that homogentisic acid is an intermediate in the conversion of phenylalanine and tyrosine to acetoacetate is indicated by many experiments with humans (l-5), animals (6-9), and tissue preparations (lO-13), no direct evidence has been reported concerning the mechanism of its oxidation. However, the formation of /?-ketoadipic acid from phenol in the presence of cholera Vi...