Interaction of chlormezanone enantiomers with rat liver microsomes

Abstract

Both chlormezanone enantiomers, for the first time obtained by enantiospecific HPLC with a 100% yield, bind to oxidized cytochrome P-450 in rat liver microsomes with a binding curve according to type I, similar to hexobarbital but less pronounced. There are no differences between the binding curves of the two enantiomers. Ethylmorphine N-demethylation, ethoxycoumarin and ethoxyresorufin O-deethylation are inhibited by both chlormezanone enantiomers at 0.1-1 mM concentrations: no differences could be found. Luminol and lucigenin amplified chemiluminescence indicating the formation of reactive oxygen species was not influenced by either enantiomer in concentration ranges between millimolar and micromolar, whereas hydrogen peroxide formation was inhibited. NADPH/Fe stimulated lipid peroxidation was not influenced. Scavenger activity could not be demonstrated: the zymosan stimulated whole blood chemiluminescence was not influenced significantly.

Molecular Docking, Synthesis of Novel Schiff Base 1, 3-Thiazine Compounds from 3-Methoxy Chalcone and Evaluation of Their Anxiolytic Activity

“…1 It was discovered that 1,3-thiazines are six-membered heterocyclic rings that include sulfur and nitrogen,is a potential pharmacophore,and are rather stable in other compounds with significant medical applications, for eg, chlormezanone (used a muscle relaxant and as an anxiolytic). 2 Results from studies using thiazine derivative moiety have revealed a variety of biological and pharmacological characteristics, including anticonvulsant, 3 antibacterial, 4 COX-2 inhibitors, 5 NSAID, 6 anticancer, [7][8] antidiabetic, 9 anesthetic, 10 and other actions. Over the world, treating bacterial infections provides a substantial therapeutic challenge.…”

Investigations of Interactions of Chlormezanone Racemate and Its Enantiomers on Human Keratinocytes and Human Leucoytes in vitro

“…500 mm (Daicel, Tokyo, Japan), UV detector at 254 nm, eluent n-hexane/EtOH (1/1, v/v), flow 70 ml/min. Yield was 100%, chromatographic purity [14,16,17].…”