. "2"^^ . . . "Phosphonates Acyclic nucleoside phosphonates ANP Nucleotides Nucleotide analogs Antivirals Prodrugs Bioavailability Peptidomimetics"@en . . "Byla vypracov\u00E1na metodika synt\u00E9zy dipeptidick\u00FDch a aminokyselinov\u00FDch profarmak r\u016Fzn\u00FDch typ\u016F acyklick\u00FDch nukleosidfosfon\u00E1t\u016F a vzorky testov\u00E1ny na protivirovou aktivitu. Tyrosinov\u00E9 estery a tyrosinamidov\u00E9 deriv\u00E1ty alkylovan\u00E9 dlouh\u00FDmi mastn\u00FDmi \u0159et\u011Bzci byly z farmakologick\u00E9ho hlediska shled\u00E1ny jako nejoptim\u00E1ln\u011Bj\u0161\u00ED pro dal\u0161\u00ED v\u00FDvoj vzhledem k vysok\u00E9 stabilit\u011B v plasm\u011B a dobr\u00E9 biodostupnosti."@cs . "New synthetic methodology leading to dipeptide and amino acid prodrugs of various acyclic nucleoside phosphonates has been worked out and the samples tested for antiviral activity. For further development, tyrosine esters and long chain alkylated tyrosine amide derivatives were found the most optimal from a pharmacological view point due to a high plasma stability and good bioavailability."@en . "2013-06-28+02:00"^^ . "Transformation of acyclic nucleoside phosphonates (ANPs) to appropriate prodrugs helps to improve their low bioavailability connected with a limited transport through the cell membrane caused by a presence of negative charges in the molecule. The advantage of peptidomimetic prodrugs is releasing of an active compound in target tissue together with a completely nontoxic and natural accompanying material as by-product. Development of orally active peptide drugs is often limited by their unfavorable physicochemical properties. However, their appropriate structural modifications to form peptidomimetics, especially modifications increasing the hyhobicity but simultaneously decreasing the hydrogen bonding potential open the way to circumvent metabolic enzymes and improve their oral bioavailability. In the field of ANPs we will focus to strategy originally developed in McKenna\u2019s group based on esterification of ANPs with a side-chain hydroxyl group of some serine containing dipeptides."@en . . . "Preparation of Peptidomimetic Prodrugs of Acyclic Nucleoside Phosphonates as Antivirals with Improved Bioavailability"@en . "2010-05-01+02:00"^^ . . "0"^^ . "2012-12-31+01:00"^^ . . "P\u0159\u00EDprava peptidomimetick\u00FDch profarmak acyklick\u00FDch nukleosidfosfon\u00E1t\u016F jako antivirotik se zv\u00FD\u0161enou biologickou vyu\u017Eitelnost\u00ED" . . . "http://www.isvav.cz/projectDetail.do?rowId=ME10040"^^ . . . . "ME10040" . . "1"^^ . "C\u00EDlem projektu je synt\u00E9za nov\u00E9ho typu netoxick\u00FDch profarmak acyklick\u00FDch nukleosidfosfon\u00E1t\u016F s modifikovan\u00FDm dipeptidov\u00FDm zbytkem a na z\u00E1klad\u011B studia jejich farmakokinetick\u00FDch vlastnost\u00ED v\u00FDb\u011Br kandid\u00E1t\u016F pro potenci\u00E1ln\u00ED v\u00FDvoj budouc\u00EDho l\u00E9\u010Diva." . . . . . "2012-02-16+01:00"^^ . "0"^^ . . "2"^^ . .