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Determination of Inhibiting Properties, Hydrolytic Stability and Partition Coefficients of Dialkylcarbamates.
Authors: Štěpánková Šárka | Zdražilová Pavla | Komers Karel | Čegan Alexander | Ventura Karel
Year: 2004
Type of publication: ostatní - přednáška nebo poster
Name of source: The 2004 Youger European Chemists´ Conference
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Language Name Abstract Keywords
cze Stanovení inhibičních vlastností, hydrolytické stability a rozdělovacího koeficientu dialkylkarbamátů. Byla testována inhibiční schopnost nových inhibitorů hydrolýzy acetylthiocholinu acetylcholin- a butyrylcholinesterázou, a to měřením jejich indexu pI50, rychlostních konstant k a aktivační energie hydrolýzy E , jejich hydrolytické stability a rozdělovacích koeficientů v systému voda : oktan = 1 : 1. Byly testovány deriváty N,N´-dialkyl-3 (diethylamino)fenolu, podobné svou strukturou oficiálnímu léku Alzheimerovy choroby Rivastigminu-Exelonu. Měření byla prováděna v oboru pH 7.6 ? 9.6 při různých teplotách Ellmanovou spektrální metodou. Byly sestrojeny závislosti log k vs. pH, resp. 1/T a E vs. počet atomů uhlíku v alkylskupině. Bylo zjištěno, že všechny testované karbamáty jsou únými inhibitory obou cholinesteráz, jejich hydrolytická stabilita je přiměřená, ale jsou málo lipofilní. inhibitor, enzyme, acetylcholinesterase, butyrylcholinesterase
eng Determination of Inhibiting Properties, Hydrolytic Stability and Partition Coefficients of Dialkylcarbamates. The aim of the research was to find a suitable inhibitor decreasing the concentration and/or activity of acetylcholine esterase (ACHE) and/or butyrylcholinesterase (BCHE) and to determine its hydrolytic stability and partition coefficient in system water:octane-1-ol. The inhibiting power of chosen substances owing to the hydrolysis of acetylthiocholine by butyrylcholinesterase or acetylcholinesterase was tested. N,N-dialkyl derivatives of 3-(diethylamino)phenol belong to the group of carbamate cholinesterase inhibitors and their structure is very similar to the structure of drug used for treatment Alzheimer´s disease ? rivastigmine (Exelon?). The force of every substance inhibiting an enzyme can be approximately evaluated by its index pI50. For determination of pI50 the spectrophotometric Ellman´s method was used. Kinetics of hydrolysis of N,N-dialkyl derivatives of 3-(diethylamino)phenol was observed. All kinetic measurements were carried out spectrophotometrically. Hydrolytic velocity constants k and activation energy E of selected compounds in the pH range 7,6 ? 9,6 were determined. The dependecies of log k vs. pH (pH profile), E vs. number of carbon atoms in alkyl group, log k vs. 1000/T were constructed. The partition coefficients of chosen substances in system water:octane-1-ol were determined. It has been proved that chosen carbamates are effective cholinesterase inhibitors, their hydrolytic stability is adequate but rate of their lipophility is quite low. inhibitor, enzyme, acetylcholinesterase, butyrylcholinesterase

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