77875-91-3Relevant academic research and scientific papers
Synthesis of tricarbonyl rhenium and technetium complexes of a 5′-carboxamide 5-ethyl-2′-deoxyuridine for selective inhibition of herpes simplex virus thymidine kinase 1
Desbouis,Schubiger,Schibli
, p. 1340 - 1347 (2008/02/04)
Herpes simplex virus thymidine kinase type 1 (HSV1-TK) is frequently used as reporter protein in gene therapy. Our aim is to produce single photon emitting reporter probe based on technetium-99m. The synthesis of organometallic technetium and rhenium comp
Design and studies of novel 5-substituted alkynylpyrimidine nucleosides as potent inhibitors of mycobacteria
Rai, Dinesh,Johar, Monika,Manning, Tracey,Agrawal,Kunimoto, Dennis Y.,Kumar, Rakesh
, p. 7012 - 7017 (2007/10/03)
We herein report a new category of 5-substituted pyrimidine nucleosides as potent inhibitors of mycobacteria. A series of 5-alkynyl derivatives of 2′-deoxyuridine (1-8), 2′-deoxycytidine (9-14), uridine (15-17), and 2′-O-methyluridine (18, 19) were synthe
2'-deoxy-5-ethynyluridine-3',5'-diestens for treatment of VZV and CMV infections
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, (2008/06/13)
The present invention relates to the use of 2'-deoxy-5-ethynyluridine and its pharmaceutically acceptable derivatives in the treatment and prophylaxis of varicella zoster virus and cytomegalovirus infections. Also provided are pharmaceutical formulations
Nucleic Acid Related Compounds. 39. Efficient Conversion of 5-Iodo to 5-Alkynyl and Derived 5-Substituted Uracil Bases and Nuleosides
Robins, Morris J.,Barr, Philip J.
, p. 1854 - 1862 (2007/10/02)
Coupling of terminal alkynes with 5-iodo-1-methyl-uracil and 5-iodouracil nucleosides (protected as their p-toluyl esters) proceeded in high yields in the presence of bis(triphenylphosphine)palladium(II) chloride and copper(I)iodide in warm triethylamine.Several of the subsequently deprotected 5-alkynyl-2'-deoxyuridines, including the parent 5-ethynyl-2'-deoxyuridine, had antiviral activity, and their 5'-monophosphates inhibited thymidylate synthetase.Hydrogenation of the 5-alkynyl side chain can be controlled to give (Z)-5-alkenyl- or the saturated 5-alkyl-2'-deoxyuridines.This provides a stereocontrolled route to the known 5-ethyl-and 5-n-hexyl-2'-deoxyuridines as well as (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU).Hydration of the triple bond gave the corresponding uracil-5-alkanone products in favorable cases.
NUCLEIC ACID RELATED COMPOUNDS. 31. SMOOTH AND EFFICIENT PALLADIUM-COPPER CATALYZED COUPLING OF TERMINAL ALKYNES WITH 5-IODOURACIL NUCLEOSIDES
Robins, Morris J.,Barr, Philip J.
, p. 421 - 424 (2007/10/02)
Coupling of terminal alkynes with protected 5-iodouracil nucleosides in the presence of dichlorobis(triphenylphosphine)palladium and copper(I) iodide in triethylamine gives the corresponding 5-(alkyn-1-yl)uracil nucleosides in 72-92percent yields.
