Proteins are useful chiral selectors. In order to understand the recognition mechanism and discrimination, binding of (R)- (S)-enantiomers a series designed amino alcohol inhibitors based on propranolol cellobiohydrolase Cel7A (Trichoderma reesei) has been studied more closely. X-ray crystal structures were determined protein complex with strongest analogue. The combination structural data, the...

BACKGROUND Halothane is made and used as a racemate (an equimolar mixture of R- and S- enantiomers). This study was initiated to determine whether there were demonstrable enantiomeric differences in the whole-body pharmacokinetics of halothane that might have significance for studies in which racemate is used. METHODS Adult male Wistar rats were exposed to halothane vaporized in the atmospher...

The research into the separation of drug enantiomers is closely related to the safety and efficiency of the drugs. The aim of this study was to develop a simple and validated HPLC method to analyze cetirizine enantiomers. In the case of liquid dosage forms, besides the active substance in large amounts there are usually also inactive ingredients such as methyl- and propylparaben. Unfortunately,...

Hydroxysteroid (alcohol) sulfotransferase STa catalyzes the 3'-phosphoadenosine 5'-phosphosulfate-dependent O-sulfonation of a diverse array of alcohols including neutral hydroxysteroids. Many of the secondary alcohols that interact with this sulfotransferase are the metabolic products of stereoselective oxidation or reduction reactions. The role that the stereochemistry of secondary alcohol su...

We assessed (1) whether the enantiomers of terpinen-4-ol, odorants that activate nearly identical areas of the olfactory bulb, are more difficult to discriminate than those of carvone, odorants that activate different areas of the olfactory bulb, and (2) whether olfactory bulb lesions that disrupt the pattern of bulbar activation produced by these enantiomers degraded the ability of rats to dis...

in recent years there has been considerable interest in the synthesis and separation of enantiomers of organic compounds especially because of their importance in the biochemistry and pharmaceutical industry. high-performance liquid chromatography is a very useful method for the direct separation of enantiomers. however, about 30−40 years ago, commercially available chiral stationary phases wer...

A common approach in resolving enantiomers of chiral basic drugs by capillary electrophoresis (CE) is to use cyclodextrins (especially their anionic derivatives) as chiral selector in the acidic buffer (pH ≤ 3) in normal or reversed (carrier) mode. Then, some organic modifiers are added to the buffer solution if the resolution is not satisfactory. In case of cetirizine (CTN), applying the same ...

To identify which cytochrome P-450 (CYP) isoform(s) are involved in the major pathway of disopyramide (DP) enantiomers metabolism in humans, the in vitro formation of mono-N-desalkyldisopyramide from each DP enantiomer was studied with human liver microsomes and nine recombinant human CYPs. Substrate inhibition showed that SKF 525A and troleandomycin potently suppressed the metabolism of both D...

Two enantiomers of carbovir, a carbocyclic analog of 2',3'-dideoxyguanosine, were compared with respect to their phosphorylation and the phosphorylation of their nucleotides by mammalian enzymes. 5'-Nucleotidase catalyzed the phosphorylation of (-)-carbovir, which is active against HIV (human immunodeficiency virus), but did not phosphorylate (+)-carbovir. (-)-Carbovir monophosphate was 7,000 t...

Chiral drug naftopidil (NAF), a specific α1D-adrenoceptor (AR) antagonist for the treatment of benign prostatic hyperplasia, was used in racemic form for several decades. Our recent work declared that NAF enantiomers showed the same antagonistic effects on the α1D-AR, but the binding mechanism of these two stereochemical NAF isomers to the α1D receptor remained unclear. Herein, we reported the ...