A series of 2-(4-phenylpiperazin-1-yl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors (AChEIs) were designed and synthesized for the treatment Alzheimer’s disease (AD). Their bioactivities evaluated by Ellman’s method, results showed that most compounds displayed moderate inhibitory activities in vitro. Among them, compound 6g exhibited potent activity against AChE with ...

Cells maintain cellular homeostasis employing different regulatory mechanisms to respond external stimuli. We study two groups of signal-dependent transcriptional regulatory mechanisms. In the first group, we assume that repressor and activator proteins compete for binding to the same regulatory site on DNA (competitive mechanisms). In the second group, they can bind to different regulatory reg...

Assuming complete hepatic substrate metabolism and system linearity, quantitative effects of in vivo competitive inhibition are investigated. Following oral administration of a substrate in the presence of a competitive inhibitor, determination of the inhibition constant (Ki) is possible when plasma concentration-time profiles of both substrate and inhibitor are available. When triazolam is the...

background: diabetes mellitus is a chronic disease. decreasing postprandial hyperglycemia by retarding glucose absorption through inhibiting carbohydrates digesting enzymes (α-amylase and α-glucosidase) is one of many approaches used for the management of this disease. this study was aimed at evaluating the normoglycaemic potential of helianthus annuus leaf. methods: the effect of the in vitro ...

Antibodies to crystalline bovine hepatic L-glutamic dehydrogenase were induced in rabbits. These antibodies inhibited the bovine glutamic dehydrogenase used as antigen, and also inhibited glutamic dehydrogenases from rat, rabbit, human, pigeon, and frog livers, as well as frog renal and muscle glutamic dehydrogenase. The antibody did not inhibit yeast glutamic dehydrogenase which differs from t...

flavonoids could serve as potent inhibitors of xanthine oxidase (xo). in the present study, the effects of ruta graveolens l. extract and its major isolated flavonoids, quercetin and rutin, on guinea pig liver xo have been investigated. the inhibitory effects of r. graveolens, quercetin and its glycoside form, rutin, were assayed spectrophotometrically. r. graveolens extract showed moderate inh...