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	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
	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
	Use of 1,3-dioxolanes in the syntheses of alpha-branched alkyl and aryl N-9-[2-(phosphonomethoxy)ethyl]purines Pomeisl, Karel ; Holý, Antonín ; Krečmerová, Marcela Syntheses of various alkyl and aryl substituted N-9-[2-(phoshonomethoxy)ethyl]purines from a number of 2-alkyl(aryl)-1,3-dioxolanes were developed in preparative yields. The cleavage of a dioxolane ring with Lewis acids was chosen for preparation of suitable phosphonate building blocks as a key reaction step followed by their Mitsunobu reaction with purine bases. Obtained phosphonate derivatives were tested as potential HG(X)PRTase inhibitors. In contrast to previously published N-9-[2-(phosphonoethoxy)ethyl]purines, no inhibitory activity towards this enzyme was observed. Detailed record
	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. Detailed record
	Nové virostatikum, 1-(S)-[3-hydroxy-(2-phosphonomethoxy)propyl]-5-azacytosin: estery a modifikované baze Krečmerová, Marcela ; Holý, Antonín ; Pískala, Alois ; Andrei, G. ; Snoeck, R. ; Balzarini, J. ; De Clercq, E. A series of 6-alkyl-HPMP-5azaC was synthesized using ammonia mediated ring-opening reaction of protected HPMP-5-azaC ester followed by condensation reaction with orthoesters and deprotection of ester groups. Introduction of long chain acyl groups to the N4-position was performed using reaction of some acyl chloride (e.g. behenoyl chloride) and appropriate ester of HPMP-5-azaC or its cyclic form. Detailed record
	Syntéza C-5 substituovaných derivátů HPMPC (Cidofoviru) Krečmerová, Marcela ; Holý, Antonín The series of N4-alkyl derivatives of (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-ethylcytosine was prepared from the corresponding 5-ethyl-4-methoxypyrimidin-2-(1H )-one intermediates by the action of primary amines. Sonogashira coupling was used for the preparation of 5-ethynyl HPMPC. Detailed record

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