. "1. P\u0159\u00EDnosem projektu byla synt\u00E9za \u0159ady chemicky i biochemicky zaj\u00EDmav\u00FDch l\u00E1tek. Bohu\u017Eel, \u017E\u00E1dn\u00E1 z nich nevykazovala o\u010Dek\u00E1van\u00FD reaktiva\u010Dn\u00ED efekt na acetylcholinesterazu. 2. Charakteristiska v\u00FDsledk\u016F v z\u00E1v\u011Bre\u010Dn\u00E9 kart\u011B je adekv\u00E1tn\u00ED. 3. Na \u0159e\u0161en\u00ED projektu se"@cs . "1"^^ . "Probl\u00E9m reaktivace acetylcholinester\u00E1zy inhibovan\u00E9 toxick\u00FDmi agrochemik\u00E1liemi (nap\u0159. Paraoxon, Parathion a pod.) \u010Di chemick\u00FDmi zbran\u011Bmi jako je Sarin, Soman, VX atd. je st\u00E1le aktu\u00E1ln\u00ED. Navrhovan\u00FD projekt je zam\u011B\u0159en na synt\u00E9zu nov\u00FDch typ\u016F reaktiv\u00E1tor\u016F acetylcholinester\u00E1zy a na testov\u00E1n\u00ED jejich \u00FA\u010Dinnosti. Slou\u010Deniny, jejich\u017E synt\u00E9za je pl\u00E1nov\u00E1na, lze rozd\u011Blit podle jejich struktury do dvou z\u00E1kladn\u00EDch skupin. V prvn\u00ED z nich jsou l\u00E1tky, u nich\u017E je zachov\u00E1na hydroxyiminoskupina jako \u00FA\u010Dinn\u00FD nukleofil defosforyluj\u00EDc\u00ED serinovou hydroxyskupinu v aktivn\u00EDm centru enzymu. Ve druh\u00E9 skupin\u011B jsou l\u00E1tky, ve kter\u00FDch je navrhov\u00E1na jako nukleofil hydroxyskupina v gemin\u00E1ln\u00EDch diolech. U t\u011Bchto l\u00E1tek se p\u0159edpokl\u00E1d\u00E1 reaktivace acetylcholinester\u00E1zy prob\u00EDhaj\u00EDc\u00ED v katalytick\u00E9mcyklu. P\u0159ipraven\u00E9 l\u00E1tky budou testov\u00E1ny in vitro pomoc\u00ED experiment\u016F s enzymem inhibovan\u00FDm modelovou toxickou organickou slou\u010Denino fosforu. P\u0159edpokl\u00E1d\u00E1 se, \u017Ee z\u00EDskan\u00FDch v\u00FDsledk\u016F bude mo\u017Eno u\u010Dinit obecn\u00E9 z\u00E1v\u011Bry ve smyslu struktura-\u00FA\u010Dinnost." . . "GA203/96/1585" . . "The problem of the reactivation of acetlycholinesterase inhibited by phosphorylation either by toxic agrochemicals (e.g. Paraoxon, Parathion etc.) or by chemical weapons as Sarin, Soman, VX etc. is still relevant The proposed project is directed to the synthesis of new types of reactivators of acetylcholinesterase and evaluation of their efficiency. The intended compounds can be divided into two main groups according to their structures. In the first one the hydroxyimino group as the efficient nucleophile dephosphorylating the serine hydroxy group in the active centre of the enzyme is maintained. In the second one, hydroxy group in geminal diols is proposed as a new nucleophile. These compounds are expected to raectivate the acetylcholinesterase in a catalytic cycle. The prepared substances will be tested in vitro experiments using the enzyme inhibited by model organophosphorous poisons. General conclusions in terms of structure-activity relationships are expected to be done from the otained results."@en . "1"^^ . . "0"^^ . . "1"^^ . . . . . . "http://www.isvav.cz/projectDetail.do?rowId=GA203/96/1585"^^ . . . "Reaktiv\u00E1tory acetylcholinester\u00E1zy" . . . . "0"^^ . "Reactivators of acetylcholinesterase"@en . .