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	Příprava 8-C-substituovaných acyklických nukleosidfosfonátů odvozených od 2,6 diaminopurinu s využitím Negishiho cross-couplingu Sedláček, Ondřej ; Pohl, Radek ; Holý, Antonín 8-Allyl-, cyclopropyl-, trifluoromethyl-, cyano-, carbethoxy- and acetaldehydo-2,6-diamino- 9-[2-(phosphonomethoxy)ethyl]purine (PMEDAP) were prepared by Negishi cross-coupling of the 8-bromo-PMEDAP under catalysis with Pd2dba3 with various phosphine ligands followed by deprotection. Detailed record
	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. 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
	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. Detailed record
	Snadné syntézy pyrimidinových acyklických nukleosidfosfonátů a jejich potenciál v biomedicinálních aplikacích Pomeisl, Karel ; Holý, Antonín ; Votruba, Ivan ; Nencka, Radim ; Pohl, Radek The presented syntheses using a nucleophilic fluorination, Suzuki–Miyaura coupling reactions and phosphorylation were successfully applied for the preparation of a number of pyrimidine acyclic nucleoside phosphonates in connection of finding of potential bioactive compounds. Detailed record
	Efektivní syntézy acyklických nukleosidfosfonátů s jedním otevřeným a jedním nově uzavřeným kruhem Jansa, Petr ; Dračínský, Martin ; Holý, Antonín In order to study the SAR, we prepared new 6-[2-(phosphonomethoxy)ethoxy]-2,4-diaminopyrimidine (PMEO-DAPy) analogues substituted by another ring between positions 4 and 5. Detailed record
	Příprava N9-(3-fluoro-2-phosphonomethoxypropyl) (FPMP) derivátů N6-substituovaných adeninů a 2,6-diaminopurinů Baszczyňski, Ondřej ; Holý, Antonín ; Dračínský, Martin ; Klepetářová, Blanka An efficient method of the synthesis N9-(3-fluoro-2-phosphonomethoxypropyl) (FPMP) derivatives of purine bases was developed. A series of N6-substituted FPMP dervatives of purine and 2-aminopurine were prepared by using this method. Detailed record
	Analoga pyrimidine-2-on nukleosidů a jejich enzymatická galaktosylace Blažek, Jiří ; Holý, Antonín ; Lipová, P. ; Purkrtová, Z. ; Králová, B. A series of acyclic nucleoside analogs of pyrimidine-2-one were glykosylated via enzymatic route with beta-D-galactosidase (E.C. 3.2.1.23, beta-D-galactoside galactohydrolase) from Arthrobacter sp. C 2-2. Detailed record
	Metalace 6-halo-2,4-dimethoxypyrimidinů jako klíčový krok pro syntézu biologicky aktivních sloučenin Nencka, Radim ; Hřebabecký, Hubert ; Votruba, Ivan ; Dračínský, Martin ; Holý, Antonín Introduction of carbon substituents to the position C-5 and C-6 of uracil ring was performed by reaction of organometallic derivatives of uracil with electrophiles or by transition metal catalyzed cross-coupling reaction. Especially lithiathion was studied intensively. 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

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