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	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
	A novel, highly stereoselective synthetic approach for the preparation of substituted 2,5-dihydro-2,5-dihydroxyfurans Jansa, Petr ; Kaiser, Martin Maxmilian ; Holý, Antonín ; Janeba, Zlatko A novel highly stereoselective reduction of 5-substituted furan-2(5H)-ones has been developed as a key step in the synthesis of 2,5-dihydro-5-hydroxyfuran-2-yl nucleosides. Detailed record
	Biological properties of the C-8 substituted analogues of 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA) Janeba, Zlatko ; Holý, Antonín ; Zídek, Zdeněk The 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA) derivatives substituted at the C-8 position of the purine moiety did not exhibited any pronounced antiviral or antimalarial activity, but both 8-hydroxy and 8-sulfanyl derivatives of PMEA possess significant immunostimulatory activities. Detailed record
	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. Detailed record
	Synthesis and biological properties of the 2’-trifluoromethyl analogues of tenofovir Jansa, Petr ; Kolman, Viktor ; Janeba, Zlatko A series of acyclic nucleoside phosphonates substituted at the aliphatic part of the molecule by the trifluoromethyl group was prepared but none of the compounds exhibits any anti-HIV or anti-HCV activities. Detailed record
	Efficient one-pot synthesis of polysubstituted 6-[(1H-1,2,3-triazol-1-yl)methyl]uracils through the "click" protocol Jansa, Petr ; Špaček, Petr ; Holý, Antonín ; Votruba, Ivan ; Janeba, Zlatko Synthesis of triazoloacyclic nucleosides and nucleoside phosphonates was developed as the one-pot Cu(I)-catalyzed azide alkyne Huisgen "click" cycloaddition. A novel Cu(I)-catalyzed decarboxylation reaction of 1-substituted 1H-1,2,3-triazole-4-carboxylates at room temperature was observed and used for the preparation of 1-substituted 1H-1,2,3-triazoles. Detailed record
	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. 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

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