. . . "7"^^ . "Vyu\u017Eit\u00ED polymer\u016F jako nosi\u010D\u016F l\u00E9\u010Div (drug delivery systems) je progresivn\u00ED trend modern\u00ED farmaceutick\u00E9 chemie. Vazba na hydrofiln\u00ED polymer m\u016F\u017Ee \u0159e\u0161it z\u00E1va\u017En\u00E9 nedostatky, kter\u00E9 v\u00FDznamn\u011B omezuj\u00ED mo\u017Enosti terapeutick\u00E9ho vyu\u017Eit\u00ED mnoha biologicky aktivn\u00EDch l\u00E1tek. Nalezen\u00ED efektivn\u00ED a bezpe\u010Dn\u00E9 farmakoterapie t\u011B\u017Ek\u00FDch, \u017Eivot ohro\u017Euj\u00EDc\u00EDch syst\u00E9mov\u00FDch myk\u00F3z pat\u0159\u00ED k\u00A0v\u00FDznamn\u00FDch c\u00EDl\u016Fm dne\u0161n\u00ED v\u011Bdy. T\u011B\u017Ei\u0161t\u011Bm p\u0159edkl\u00E1dan\u00E9ho projektu je synt\u00E9za konjug\u00E1t\u016F antimykoticky aktivn\u00EDch l\u00E1tek s\u00A0hydrofiln\u00EDmi nosi\u010Di na b\u00E1zi poly(ethylenglykolu). Jako ligandy pou\u017Eijeme polyenov\u00E1 antibiotika a p\u0159\u00EDrodn\u00ED i syntetick\u00E9 slou\u010Deniny se zn\u00E1mou antifung\u00E1ln\u00ED aktivitou - laktony, substituovan\u00E9 thioamidy. Sou\u010D\u00E1st\u00ED projektu jsou syntetick\u00E9 obm\u011Bny polymern\u00EDch nosi\u010D\u016F, izolace p\u0159\u00EDrodn\u00EDch ligand\u016F, HPLC anal\u00FDza p\u0159ipraven\u00FDch konjug\u00E1t\u016F, jejich degrada\u010Dn\u00EDch produkt\u016F a biologick\u00E9ho materi\u00E1lu z\u00A0farmakokinetick\u00FDch studi\u00ED. Projekt m\u00E1 komplexn\u00ED charakter: p\u0159\u00EDprava konjug\u00E1t\u016F a jejich charakterizace pomoc\u00ED fyzik\u00E1ln\u011B-chemick\u00FDch metod; hodnocen\u00ED" . "7"^^ . "Nov\u00E9 antimykoticky aktivn\u00ED konjug\u00E1ty poly(ethylenglykol\u016F)" . . . . . "Using polymers as carriers (drug delivery systems) is a progressive trend of up-to-date medicinal chemistry. A binding of the drug to a hydrophilic polymer can solve serious shortages that significantly limit therapeutic\u00A0use of many biologically active compounds. Searching for effective and safe pharmacotherapy of severe, life-threatening systemic mycoses is one of the goals of present-day science. The project is based mainly on the synthesis of conjugates of antifungal agents and hydrophilic carriers based on poly(ethylene glycol)s. Ligands, i.e. the compounds with known antifungal properties, will be polyene antibiotics, lactones, and substituted thioamides. Synthetic modifications of carriers, isolation of natural ligands, and HPLC assay of conjugates, their degradation products, and biological samples will be also performed. The nature of the project is complex: preparation of conjugates and their chemical characterization; evaluation of their in vitro antifungal activity, in vitro"@en . " pegylation" . . . . . "The grant project aimed to synthesize macromolecular drug carriers based on modified poly(ethylene glycols) and to produce their conjugates with amphotericin B as novel antimycotically active substances. The prepared conjugates of different types underwe"@en . . "drug delivery systems; pegylation; poly(ethylene glycol); antifungal activity; pharmacokinetics"@en . "0"^^ . . "1"^^ . "1"^^ . "\u00DAkolem grantov\u00E9ho projektu bylo syntetizovat makromolekul\u00E1rn\u00ED nosi\u010De l\u00E9\u010Div na b\u00E1zi modifikovan\u00FDch poly(ethylenglykol\u016F) a p\u0159\u00EDpravit jejich konjug\u00E1ty s amfotericinem B jako nov\u00E9 antimykoticky \u00FA\u010Dinn\u00E9 l\u00E1tky. P\u0159ipraven\u00E9 konjug\u00E1ty r\u016Fzn\u00FDch typ\u016F byly podrobeny i"@cs . . "2006-01-01+01:00"^^ . "2009-10-22+02:00"^^ . " poly(ethylene glycol)" . "2008-04-25+02:00"^^ . "drug delivery systems" . " antifungal activity" . . . . "2008-12-31+01:00"^^ . . "Novel antifungally active conjugates of poly(ethylene glycol)s"@en . . "GA203/06/0583" . . "http://www.isvav.cz/projectDetail.do?rowId=GA203/06/0583"^^ .