National Repository of Grey Literature 32 records found  beginprevious20 - 29next  jump to record: Search took 0.00 seconds. 
9-[2-hydroxy-3-(phosphonomethoxy)propyl] ("iso-HPMP")derivatives of purine bases and their side-chain modified analogues: synthesis and antimalarial activity
Krečmerová, Marcela ; Holý, Antonín ; Hocková, Dana ; Dračínský, Martin ; Keough, D. T. ; Guddat, L. W.
Hypoxanthine and guanine iso-HPMP derivatives substsituted in 2´-position were prepared and studied as potential inhibitors of a key enzyme of the malarial parasite Plasmodium falciparum HGXPRT.
Piperidine nucleoside phosphonic acid derivatives
Kovačková, Soňa ; Dračínský, Martin ; Rejman, Dominik
A series of novel phosphonic acid derivatives of piperidine nucleosides was prepared, whereby synthesis of both enantiomeric and diastereomeric derivatives was discussed. Preparation of diphosphate analogs of phosphonic acids derivatives is also described. The prepared nucleotide analogs were tested for their potential biological properties.
3-Fluoro-2-(phosphonomethoxy)propyl hypoxanthine and guanine derivatives as inhibitors of plasmodial hypoxanthine-guanine-xanthine phosphoribosyltransferases
Baszczyňski, Ondřej ; Jansa, Petr ; Hocková, Dana ; Janeba, Zlatko ; Dračínský, Martin ; Holý, Antonín ; Keough, D. T. ; de Jersey, J. ; Guddat, L. W.
A new methodology for the synthesis of ANPs containing 9-[2-(phosphonoethoxy)ethyl] (PEE) moiety has been developed. FPEP compound containing guanine moiety exhibited inhibition activity against the enzyme in micromolar range without any signs of toxicity.
The efficient synthesis of 2-aryl substituted pyrimidine acyclic nucleoside phosphonates using Liebeskind-Srogl cross-coupling
Česnek, Michal ; Břehová, Petra ; Dračínský, Martin ; Holý, Antonín ; Janeba, Zlatko
A series of novel acyclic nucleoside phosphonates with a built-in 2-arylsubstituted pyrimidine moiety has been prepared using the Liebeskind-Srogl cross-coupling protocol. The reactions of highly functionalised 2-methylsulfanylpyrimidines with various arylboronic acids were studied and optimised.
The optimized microwave-assisted decomposition of formamides and its synthetic utility in the amination of purines and pyrimidines
Čechová, Lucie ; Jansa, Petr ; Šála, Michal ; Dračínský, Martin ; Holý, Antonín ; Janeba, Zlatko
The microwave-assisted decomposition of DMF was thoroughly studied and the reaction conditions (temperature, solvent effect, and effect of additives such as acids, bases, and salts) were optimized for its use in the amination reactions of various purines and pyrimidines.
The unique impact of microwave irradiation on the chemistry of acyclic nucleoside phosphonates
Jansa, Petr ; Holý, Antonín ; Dračínský, Martin ; Baszczyňski, Ondřej ; Česnek, Michal ; Janeba, Zlatko
Latest improvements of the syntheses of ANPs using microwave irradiation are presented, namely a novel, efficient, and environmentally friendly synthesis of dialkyl haloalkylphosphonates via the microwave-assisted Michaelis-Arbuzov reaction and microwave-assisted hydrolysis of phosphonate diesters.
Synthesis of conformationally locked carbocyclic nucleosides with norbornane as pseudosugar moiety
Dejmek, Milan ; Hřebabecký, Hubert ; Šála, Michal ; Dračínský, Martin ; Nencka, Radim
We describe the chemical synthesis of three novel structural types of conformationally locked carbocyclic nucleosides with norbornane as sugar surrogate. The presented structures bear hydroxymethyl, nucleobase or both in the bridgehead positions of the norbornane pseudosugar and thus adopt three different conformations of the cyclopentane ring – North, South, and East.
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.

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