engleski

SINTEZA I KINETIČKA ANALIZA NOVIH IMIDAZOLIJEVIH alfa-D-MANOPIRANOZIDA

It is well established that the cholinesterases, particulary butyrylcholinesterase (BChE), are associated with the patogenesis and progresion of Alzheimer’s (AD) and Parkinson’s disease (PD). Increased BChE activity plays important role in β-amyloid aggregation during the early stages of disease, thus BChE inhibition is the main target for possible therapeutic approach. ChE- inhibitors, used for palliative treatment, prevent the breakdown of acetylcholine by inhibiting enzyme in the brain regions relevent to above mentioned diseases and therby slowing neurodegradation and neural impairments.Therefore, compounds which are pseudoirreversible ChE inhibitors and interact with both active (catalytic) as well as peripheral anionic site of the enzyme, have received a great deal of attention. Compounds with attached sugar moiety have shown increased bioavailability and are easily transported across cell membranes by facilitative sugar transporters. A series of novel bicyclic imidazole α-D- mannopyranoside derivatives was synthesised and their inhibitory properties towards equine BChE studied by Ellman's method. Kinetic parameters (KM and vmax) were determined.

BChE, imidazole, synthesis, inhibition

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