66392-60-7Relevant academic research and scientific papers
Some 6-aza-5-substituted-2'-deoxyuridines show potent and selective inhibition of herpes simplex virus type 1 thymidine kinase
Basnak,Sun,Hamor,Focher,Verri,Spadari,Wroblowski,Herdewijn,Walker
, p. 187 - 206 (2007/10/03)
The synthesis and X-ray crystal structures of a series of 5- substituted-6-aza-2'-deoxyuridines is reported. These nucleoside analogues inhibit the phosphorylation of thymidine by HSV-1 TK but have no effect on the corresponding human enzyme. Detailed examination of one analogue proves it to be a competitive inhibitor of thymidine with a Ki of 0.34 μM and is a very poor substrate. The analogues are not substrates for the enzyme and also do not inhibit the degradation of thymidine by thymidine phosphorylase. Molecular modelling showed that the inhibitors fit well in the active site of HSV-1 TK, provided the conformation of the sugar moiety is the same for thymidine in the complex.
Syntheses of Thiazolo- and Thiazinotriazinones
Arndt, Friedrich,Franke, Wilfried,Klose, Walter,Lorenz, Joerg,Schwarz, Katica
, p. 1302 - 1307 (2007/10/02)
The syntheses of the thiazolo- and thiazinotriazinones 3 - 6 are described.Preparations of compounds 3 and 5 were achieved regiospecifically by using the compounds 12 and 13.
