Synthesis, SAR and molecular docking study of novel non-β-lactam inhibitors of TEM type β-lactamase.

The novel classes of acylated phenoxyanilide and thiourea compounds were investigated for their ability to inhibit TEM type β-lactamase enzyme. Two compounds 4g and 5c reveal the inhibition potency in micromolar range and show their action by non-covalent binding in the vicinity of the TEM-171 active site. The structure activity relationship around carbon chain length and different substituents in ortho- and para-positions of acylated phenoxyanilide as well as molecular modelling study has been performed.

Glucural (amigluracyl) improves survival of isolated rat hepatocytes in suspension.

Nonsteroid anti-inflammatory drug glucural (water-soluble N-methyl-D-glucosamine complex with 6-methyluracyl) improves survival of isolated rat hepatocytes stored in suspension. This effect of glucural is presumably explained by its membranotropism.

Superoxide anion production by the mitochondrial respiratory chain of hepatocytes of rats with experimental toxic hepatitis.

The progression of toxic hepatitis is accompanied by the activation of oxidative processes in the liver associated with an enhancement of the mitochondrial respiratory chain activity and superoxide anion production (O(2)(*-)). The purpose of this study was to examine our previously formulated assumption concerning the predominant contribution of the complex I to O(2)(*-) production increase by the mitochondrial respiratory chain of hepatocytes in toxic hepatitis (Shiryaeva et al. Tsitologiia, 49, 125-132 2007).

Hepatocyte mitochondrion electron-transport chain alterations in CCl(4) and alcohol induced hepatitis in rats and their correction with simvastatin.

The goal of this study was to examine the state of hepatocyte mitochondrial respiratory chain of rats with toxic hepatitis induced by CCl(4) and ethanol. Oxygen consumption by hepatocytes and mitochondria was determined. Endogenous oxygen consumption by pathological hepatocytes was 1.