Načrtovanje, sinteza in vrednotenje novih piperidinov kot potencialnih zaviralcev butirilholin-esteraze in monoamin-oksidaze B

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Jezik:	Slovenski jezik
Leto izida:	2015
Tipologija:	2.09 - Magistrsko delo
Organizacija:	UL FFA - Fakulteta za farmacijo
Založnik:	[J. Lipušček]
UDK:	543.057:616.894(043.3)
COBISS:	3981681
Št. ogledov:	1398
Št. prenosov:	236
Ocena:	0 (0 glasov)
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Sekundarni jezik:	Angleški jezik
Sekundarni naslov:	Design, synthesis and evaluation of novel pyperidines as potential butyrylcholinesterase and monoamine oxidase B inhibitors
Sekundarni povzetek:	With increased life expectancy the number of people with Alzheimer disease is growing. Consequently, new approaches for treatment of Alzheimer's disease are being developed. Concentration and enzymatic activity of BChE in the brain of a patient with Alzheimer’s disease increases with the deterioration of the disease and is responsible for the breakdown of most of acetylcholine, a neurotransmitter responsible for memory and learning. Neuroprotective properties are also very important in Alzheimer disease treatment and are a result of MAO-B inhibition. There are many different factors involved in developing Alzheimer’s disease and therefore multi-target molecules are interesting as new treatment strategies. With this in mind we synthesised and evaluated molecules with both BChE and MAO-B inhibition properties. We synthesized 6 piperidine compounds and evaluated their ChE and MAO-B inhibition. BChE and MAO-B selective inhibition was desired. Molecules were 1,3-disubstituted and 1,4-disubstituted piperidines with -H, -(CH2)2-OMe or -(CH2)3-OMe as a substituent on the sulfonamide. N-propargylic group is required for MAO-B inhibiton. Compound 6 was evaluated as a selective BChE inhibitor with IC50 = 2559,7 nM, and MAO-B inhibitor with IC50 = 43,93 μM. Compound 6 also has all the necessary physicochemical properties that are required to predict successful blood-brain barrier permeability. This compound represents a promising new lead compound for further optimisation.
Sekundarne ključne besede:	Alzheimerjeva bolezen;
Vrsta dela (COBISS):	Magistrsko delo/naloga
Komentar na gradivo:	Univ. Ljubljana, Fak. za farmacijo
Strani:	VI, 49 f.
ID:	12050949