National Repository of Grey Literature 22 records found  1 - 10nextend  jump to record: Search took 0.00 seconds. 
Konformace pyrrolidinového kruhu v pyrrolidinových analozích nukleotidů
Pohl, Radek ; Buděšínský, Miloš ; Rejman, Dominik ; Kočalka, Petr ; Rosenberg, Ivan
Molecular modeling methods were used for conformation study of pyrrolidine ring in the series of pyrrolidine nucleotide analogues. Theoretical results were compared with experimental ones obtained by NMR conformation analysis.
Příprava 8-C-substituovaných acyklických nukleosidfosfonátů odvozených od 2,6 diaminopurinu s využitím Negishiho cross-couplingu
Sedláček, Ondřej ; Pohl, Radek ; Holý, Antonín
8-Allyl-, cyclopropyl-, trifluoromethyl-, cyano-, carbethoxy- and acetaldehydo-2,6-diamino- 9-[2-(phosphonomethoxy)ethyl]purine (PMEDAP) were prepared by Negishi cross-coupling of the 8-bromo-PMEDAP under catalysis with Pd2dba3 with various phosphine ligands followed by deprotection.
Nukleosidy a nukleotidy obsahující 8-aza-7,9-dideazaxanthin
Mařák, David ; Otmar, Miroslav ; Dračínský, Martin ; Votruba, Ivan ; Holý, Antonín
The described preparation of 8-aza-7,9-dideazaxanthine from 1,3-dibenzyluracil and TosMIC was improved by using AlCl3 for final debenzylation. Treatment of 6-dibromomethyl- 5-formyluracil with benzyl-, 4-methoxybenzyl-, and 1-adamantylamine gave the corresponding 8-alkyl-8-aza-7,9-dideazaxanthines. N1- and N8-(8-phosphonooctyl)-8-aza-7,9-dideazaxanthines were prepared and found as inhibitors of thymidine phosphorylase (V79 cells, human placenta, Escherichia coli). IC50 values ranged at 3–27 .mu.M.
Studium chemické stability antivirově aktivních 5-azacytosin acyklických nukleosidfosfonátů pomocí NMR spektroskopie
Dračínský, Martin ; Krečmerová, Marcela ; Holý, Antonín
Hydrolytic decomposition of four 5-azacytosine acyclic nucleoside phosphonates was studied. Products of the decomposition are carbamoylguanidine derivatives. Stability and decomposition products of HPMP-5-azaC (a 5-azacytosine derivative with strong antiviral activity) differ from the other derivatives.
Syntézy látek mimikujících acyklické nukleosiddifosfáty
Doláková, Petra ; Dračínský, Martin ; Holý, Antonín
A series of acyclic nucleoside diphosphate mimics bearing purine and pyrimidine bases was prepared by Mitsunobu reaction of protected heterocyclic bases with appropriate alcohol containing stable diphosphate analogue.
Snadné syntézy pyrimidinových acyklických nukleosidfosfonátů a jejich potenciál v biomedicinálních aplikacích
Pomeisl, Karel ; Holý, Antonín ; Votruba, Ivan ; Nencka, Radim ; Pohl, Radek
The presented syntheses using a nucleophilic fluorination, Suzuki–Miyaura coupling reactions and phosphorylation were successfully applied for the preparation of a number of pyrimidine acyclic nucleoside phosphonates in connection of finding of potential bioactive compounds.
Efektivní syntézy acyklických nukleosidfosfonátů s jedním otevřeným a jedním nově uzavřeným kruhem
Jansa, Petr ; Dračínský, Martin ; Holý, Antonín
In order to study the SAR, we prepared new 6-[2-(phosphonomethoxy)ethoxy]-2,4-diaminopyrimidine (PMEO-DAPy) analogues substituted by another ring between positions 4 and 5.
Příprava N9-(3-fluoro-2-phosphonomethoxypropyl) (FPMP) derivátů N6-substituovaných adeninů a 2,6-diaminopurinů
Baszczyňski, Ondřej ; Holý, Antonín ; Dračínský, Martin ; Klepetářová, Blanka
An efficient method of the synthesis N9-(3-fluoro-2-phosphonomethoxypropyl) (FPMP) derivatives of purine bases was developed. A series of N6-substituted FPMP dervatives of purine and 2-aminopurine were prepared by using this method.
Analoga pyrimidine-2-on nukleosidů a jejich enzymatická galaktosylace
Blažek, Jiří ; Holý, Antonín ; Lipová, P. ; Purkrtová, Z. ; Králová, B.
A series of acyclic nucleoside analogs of pyrimidine-2-one were glykosylated via enzymatic route with beta-D-galactosidase (E.C. 3.2.1.23, beta-D-galactoside galactohydrolase) from Arthrobacter sp. C 2-2.
Metalace 6-halo-2,4-dimethoxypyrimidinů jako klíčový krok pro syntézu biologicky aktivních sloučenin
Nencka, Radim ; Hřebabecký, Hubert ; Votruba, Ivan ; Dračínský, Martin ; Holý, Antonín
Introduction of carbon substituents to the position C-5 and C-6 of uracil ring was performed by reaction of organometallic derivatives of uracil with electrophiles or by transition metal catalyzed cross-coupling reaction. Especially lithiathion was studied intensively.

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