120401-36-7Relevant academic research and scientific papers
C6–O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents
Hulpia, Fabian,Bouton, Jakob,Campagnaro, Gustavo D.,Alfayez, Ibrahim A.,Mabille, Dorien,Maes, Louis,de Koning, Harry P.,Caljon, Guy,Van Calenbergh, Serge
, (2020/01/13)
African trypanosomiasis, a deadly infectious disease caused by the protozoan Trypanosoma brucei spp., is spread to new hosts by bites of infected tsetse flies. Currently approved therapies all have their specific drawbacks, prompting a search for novel th
Synthesis and Properties of 2′-OMe-RNAs Modified with Cross-Linkable 7-Deazaguanosine Derivatives
Yamada, Ken,Abe, Yusuke,Murase, Hirotaka,Ida, Yuta,Hagihara, Shinya,Nagatsugi, Fumi
, p. 8851 - 8862 (2018/07/25)
Cross-linkable 7-deaza-6-vinylguanosine (ADVP) and 7-propynyl-7-deaza-6-vinylguanosine (ADpVP) derivatives were synthesized and successfully incorporated into 2′-OMe-RNA oligonucleotides by solid-phase oligonucleotide synthesis. Analysis of their cross-li
NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYERMASE
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Paragraph 0620; 0621, (2017/07/14)
The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
2-substituted 6-(het)aryl-7-deazapurine ribonucleosides: Synthesis, inhibition of adenosine kinases, and antimycobacterial activity
Malnuit, Vincent,Slavětínská, Lenka Po?tová,Nau?, Petr,D?ubák, Petr,Hajdúch, Marián,Stola?íková, Ji?ina,Sná?el, Jan,Pichová, Iva,Hocek, Michal
, p. 1079 - 1093 (2015/06/08)
Abstract A series of 6-(hetero)aryl- or 6-methyl-7-deazapurine ribonucleosides bearing a substituent at position 2 (Cl, F, NH2, or CH3) were prepared by cross-coupling reactions at position 6 and functional group transformations at p
Synthesis and evaluation of S-Acyl-2-thioethyl esters of modified nucleoside 5′-monophosphates as inhibitors of hepatitis C virus RNA replication
Prakash, Thazha P.,Prhavc, Marija,Eldrup, Anne B.,Cook, P. Dan,Carroll, Steven S.,Olsen, David B.,Stahlhut, Mark W.,Tomassini, Joanne E.,MacCoss, Malcolm,Galloway, Sheila M.,Hilliard, Catherine,Bhat, Balkrishen
, p. 1199 - 1210 (2007/10/03)
Several triphosphates of modified nucleosides (1-6) were identified as inhibitors (IC50 -0.08-3.8 μM) of hepatitis C virus RNA-dependent RNA polymerase (RdRp). Although the initial SAR developed by determining the ability of the triphosphates t
OLIGONUCLEOTIDES HAVING MODIFIED NUCLEOSIDE UNITS
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Page 108, (2010/02/04)
Disclosed are oligonucleotides and oligonucleosides that include one or more modified nucleoside units. The oligonucleotides and oligonucleosides are particularly useful as antisense agents, ribozymes, aptamer, siRNA agents, probes and primers or, when hybridized to an RNA, as a substrate for RNA cleaving enzymes including RNase H and dsRNase.
A facile and improved synthesis of tubercidin and certain related pyrrolo[2,3-d]pyrimidine nucleosides by the stereospecific sodium salt glycosylation procedure [1]
Ramasamy,Imamura,Robins,Revankar
, p. 1893 - 1898 (2007/10/02)
A simple synthesis of tubercidin, 7-deazaguanosine and 2'-deoxy-7-deazaguanosine has been accomplished using the sodium salt glycosylation procedure. Reaction of the sodium salt of 4-chloro- and 2-amino-4-chloro-pyrrolo[2,3-d]pyrimidine, 3 and 4, respectively, with 1-chloro-2,3-O-isopropylidene,5-O-(t-butyl)dimethylsilyl-α-D-ribofur nose gave the corresponding protected nucleosides 6 and 7 with β-anomeric configuration. Deprotection of 6 provided 8, which on heating with methanolic ammonia gave tubercidin in excellent yield. Functional group transformation of 7, followed by deisopropylidenation gave 2-aminotubercidin and 2-amino-7-β-ribofuranosylpyrrolo[2,3-d]pyrimidine-4(3H)-thione. Treatment of 7 with 1N sodium methoxide followed by exposure to aqueous trifluoroacetic acid, and ether cleavage furnished 7-deazaguanosine. 2'-Deoxy-7-deazaguanosine and 2'-deoxy-7-deaza-6-thioguanosine were also prepared by using similar sequence of reactions employing 4 and 1-chloro-2-deoxy-3,5-di-O-p-toluoyl-α-D-erythro-pentofuranose.
