4-Chlorobutyryl group was used as amino protective group for n(-)-alpha-phenylglycine (I). N-Hydroxysuccinimide ester III was prepared in high yield but partly racemic. Reaction of III or IV with V afforded epimeric mixtures of N,0-protected cephalexins (VI), which can be separated by crystallisation. The 4-chlorobutyryl group in VII was removed under very mild conditions giving cephalexin (IX)...

normal 0 false false false en-us x-none ar-sa background: there have been few studies to examine the effect of magnesium (mg) supplementation on liver enzymes. the aim of this study was to evaluate the effect of mg supplementation and weight loss on liver enzymes, lipid profile, and fasting blood sugar in patients with nonalcoholic fatty liver disease (nafld). materials and methods: this study ...

Dengue virus is an increasingly global pathogen. One of the promising targets for antiviral drug discovery against dengue and related flaviviruses such as West Nile virus is the viral serine protease NS2B-NS3. We here report the synthesis and in vitro characterization of potent peptidic inhibitors of dengue virus protease that incorporate phenylalanine and phenylglycine derivatives as arginine-...

Antibacterial and antifungal activity of N-phthaloylamino acid hydroxamates [C6H4(CO)2N-X-CONHOH, X=amino acid residues of glycine, beta-alanine or D-phenylglycine], was examined against 44 strains of Gram-positive and Gram-negative bacteria, and 10 species of yeasts. The level of antimicrobial activity was established using the in vitro agar assay and the standard broth dilution susceptibility...

Mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel cause cystic fibrosis. The delta F508 mutation produces defects in channel gating and cellular processing, whereas the G551D mutation produces primarily a gating defect. To identify correctors of gating, 50,000 diverse small molecules were screened at 2.5 microM (with forskolin, 20 microM) by an iodide ...

The kinetic mechanism of the reaction of D-amino acid oxidase (EC 1.4.3.3) from Trigonopsis variabilis with [alpha-1H]- and [alpha-2H]phenylglycine has been determined. The pH dependence of Vmax is compatible with pKa values of approximately 8.1 and >9.5, the former of which is attributed to a base which should be deprotonated for efficient catalysis. The deuterium isotope effect on turnover is...

An l-aminopeptidase of Pseudomonas putida, used in an industrial process for the hydrolysis of d,l-amino acid amide racemates, was purified to homogeneity. The highly l-enantioselective enzyme resembled thiol reagent-sensitive alkaline serine proteinases and was strongly activated by divalent cations. It possessed a high substrate specificity for dipeptides and alpha-H amino acid amides, e.g., ...