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	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. Úplný záznam
	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. Úplný záznam
	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. Úplný záznam
	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. Úplný záznam
	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. Úplný záznam
	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. Úplný záznam
	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. Úplný záznam

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