27999-47-9Relevant academic research and scientific papers
Design, Synthesis and Biological Evaluation of Novel Anthraniloyl-AMP Mimics as PQS Biosynthesis Inhibitors against Pseudomonas aeruginosa Resistance
Black, David StC,Das, Theerthankar,Kumar, Naresh,Rice, Scott A.,Sabir, Shekh,Subramoni, Sujatha
, (2020/07/25)
The Pseudomonas quinolone system (PQS) is one of the three major interconnected quorum sensing signaling systems in Pseudomonas aeruginosa. The virulence factors PQS and HHQ activate the transcription regulator PqsR (MvfR), which controls several activiti
Functionalized C-nucleosides as remarkable RNA binders: Targeting of prokaryotic ribosomal A-site RNA
Joly, Jean-Patrick,Gaysinski, Marc,Zara, Lorena,Duca, Maria,Benhida, Rachid
supporting information, p. 10432 - 10435 (2019/09/07)
RNA represents an extremely promising and yet challenging therapeutic target. Here, we report the design of a series of C-nucleosides as original RNA binders. Some of them bind strongly and selectively to A-site prokaryotic ribosomal RNA.
Synthesis and biological assay of new 2’-deoxyuridine dimers containing a 1,2,3-triazole linker. Part I
Michalska, Lucyna,Wawrzyniak, Dariusz,Szymańska-Michalak, Agnieszka,Barciszewski, Jan,Boryski, Jerzy,Baraniak, Dagmara
, p. 218 - 235 (2019/01/04)
We describe a simple method for the synthesis of modified dinucleosides containing pyrimidine nucleoside analogues (2’-deoxyuridine, thymidine and 5-fluoro-2’-deoxyuridine). Six different dimers with a 1,2,3-triazole linkage were obtained by azide–alkyne
Modified 5'-Trityl Nucleosides as Inhibitors of Plasmodium falciparum dUTPase
Ruda, Gian Filippo,Nguyen, Corinne,Ziemkowski, Przemyslaw,Felczak, Krzysztof,Kasinathan, Ganasan,Musso-Buendia, Alexander,Sund, Christian,Zhou, Xiao Xiong,Kaiser, Marcel,Ruiz-Perez, Luis M.,Brun, Reto,Kulikowski, Tadeusz,Johansson, Nils Gunnar,Gonzalez-Pacanowska, Dolores,Gilbert, Ian H.
scheme or table, p. 309 - 320 (2012/01/12)
2'-Deoxyuridine triphosphate nucleotidohydrolase (dUTPase) is a potential drug target for the treatment of malaria. We previously reported the discovery of 5'-tritylated analogues of deoxyuridine as selective inhibitors of this Plasmodium falciparum enzyme. Herein we report further structure-activity studies; in particular, variations of the 5'-trityl group, the introduction of various substituents at the 3'-position of deoxyuridine, and modifications of the base. Compounds were tested against both the enzyme and the parasite. Variations of the 5'-trityl group and of the 3'-substituent were well tolerated and yielded active compounds. However, there is a clear requirement for the uracil base for activity, because modifications of the uracil ring result in loss of enzyme inhibition and significant decreases in antiplasmodial action. Fewer trips to the dUMP: dUTPase is a potential drug target for the treatment of malaria. We previously reported the discovery of 5'-tritylated analogues of deoxyuridine as selective inhibitors of this P.falciparum enzyme. Herein we report further structure-activity studies of the 5'-trityl group, the introduction of various substituents at the 3'-position of deoxyuridine, and modifications of the base.
Solid-phase synthesis and evaluation of TAR RNA targeted β-carboline-nucleoside conjugates
Zhao, Peng,Jin, Hong-Wei,Yang, Zhen-Jun,Zhang, Liang-Ren,Zhang, Li-He
scheme or table, p. 3741 - 3750 (2009/02/05)
Four types of β-carboline-nucleoside conjugates were synthesized. The binding affinities of these β-carboline-nucleoside conjugates 4-11, 13 and 15 to TAR RNA were evaluated by affinity capillary electrophoresis. The data of binding affinities to TAR RNA show that conjugates 9 and 13 are stronger binders than the parent compound MC3. Computer modeling indicates that the β-carboline-nucleoside conjugate 13 can fit to the UCU three-nucleotide bulge region of TAR RNA. The Royal Society of Chemistry 2008.
Deoxyuridine triphosphate nucleotidohydrolase as a potential antiparasitic drug target
Nguyen, Corinne,Kasinathan, Ganasan,Leal-Cortijo, Isabel,Musso-Buendia, Alexander,Kaiser, Marcel,Brun, Reto,Ruiz-Pérez, Luis M.,Johansson, Nils G.,González-Pacanowska, Dolores,Gilbert, Ian H.
, p. 5942 - 5954 (2007/10/03)
This paper describes a structure-activity study to identify novel, small-molecule inhibitors of the enzyme deoxyuridine 5′-triphosphate nucleotidohydrolase (dUTPase) from parasitic protozoa. The successful synthesis of a variety of analogues of dUMP is de
Synthesis of 2'-deoxyuridine and 5-fluoro-2'-deoxyuridine derivatives and evaluation in antibody targeting studies
Henn,Garnett,Chhabra,Bycroft,Baldwin
, p. 1570 - 1579 (2007/10/02)
Derivatives of 2'-deoxyuridine and of the anticancer agent 5-fluoro-2'- deoxyuridine (FdUR) were linked indirectly via a human serum albumin carrier (HSA) to the murine antiosteosarcoma monoclonal antibody 791T/36. Starting from the 2'-deoxyuridines 1a an
Process for preparing 2-thiouracil nucleosides
-
, (2008/06/13)
Some new 1-(2- or 3-deoxy-β-D-pentofuranosyl)-2-thiouracils and 1-β-D-pentofuranosyl-2-thio-6-azauracils have been prepared. Further, it has been found that the known nucleoside compound, 1-β-D-ribofuranosyl-2-thiouracil is active against Herpes virus and against L-1210 leukemia in mice. An improved method of preparing corresponding 2-0-methyluracil and 2-0-methyl-6-azauracil intermediates is described. The method preserves the β-configuration of the starting nucleoside.
