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	New strategies in synthesis of acyclic nucleoside phosphonate prodrugs Krečmerová, Marcela ; Tichý, Tomáš ; Blažek, Jiří ; Pomeisl, Karel New syntheses of acyclic nucleoside phosphonate prodrugs including dioxolenone derivatives, functionalized alkoxyalkyl esters, utilization of hexafluorophosphate coupling agents and enzymatic glycosylations were described. Comparison of antiviral activities of diverse prodrugs was performed. Detailed record
	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. Detailed record
	Synthesis and structual assignment of novel 5´-epimeric 3´deoxy-3´,4´-didehydronucleoside-5´-C-phosphonates Petrová, Magdalena ; Buděšínský, Miloš ; Klepetářová, Blanka ; Rosenberg, Ivan Epimeric 5´-(RS) dialkyl 3-deoxy-3´,4´-didehydro-5´-C-phophonates were prepared by nucleophilic addition of various dialkyl phosphites to 3´-deoxy-3´,4´-didehydronucleoside-5´-aldehydes. Successful separation,crytstallisation and X-ray analysis of a pair of epimeric 5´-C-phosphonates, followed by correlation with a series of NMR parameters, led to efficacious configuration assignment of individual epimers in the mixtures. Detailed record
	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. Detailed record
	Chemical synthesis of prodrugs derived from 5,6-dihydro-5-azacytosine and its nucleosides using vinyl esters Janská, Lucie ; Blažek, Jiří ; Mařák, David ; Otmar, Miroslav ; Krečmerová, Marcela New strategy for synthesis of amide prodrugs without protecting groups for 5,6-dihydro-5-azacytosine and its nucleosides was developed and introduced. Vinyl esters were used as acyl donor and the reactive amino group on the heterocycle functions as nucleophile. Detailed record
	Enzymatic synthesis of ester prodrugs of DHPA and related compounds by lipases Blažek, Jiří ; Kaiser, M. M. ; Zarevúcka, Marie ; Králová, B. ; Krečmerová, Marcela An enzymatic method was used for esterification of DHPA and related compounds with vinyl esters and catalyzed by different lipases in non-aqueous media (DMF). Esters of DHPA and other compounds could be synthesized and purified in satisfactory yields. Detailed record
	Acyclic Nucleoside Phosphonates as Inhibitors of Hypoxanthine-Guanine-Xanthine Phosphoribosyltransferase: New Anti-Malarial Chemotherapy Leads Hocková, Dana ; Holý, Antonín ; Česnek, Michal ; Baszczyňski, Ondřej ; Tichý, Tomáš ; Krečmerová, Marcela ; Janeba, Zlatko ; Skinner-Adams, T. S. ; Naesens, L. ; Keough, D. T. ; de Jersey, J. ; Guddat, L. W. Hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRTase) is a widely recognized target for the discovery of new anti-malarial drugs. Specific acyclic nucleoside phosphonates (ANPs) inhibit HGXPRTase and possess anti-plasmodial activity. Within the framework of a SAR-study, the classical ANPs (e.g. PME-, PMP- and HPMP-derivatives) as well as novel series of compounds were tested to investigate their efficiency and selectivity on the inhibition of P. falciparum, P. vivax and human enzyme. Detailed record
	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. Detailed record
	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. Detailed record
	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. Detailed record

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