C6-O-alkylated 7-deazainosine nucleoside analogs: Discovery of potent and selective anti-sleeping sickness agents was written by Hulpia, Fabian; Bouton, Jakob; Campagnaro, Gustavo D.; Alfayez, Ibrahim A.; Mabille, Dorien; Maes, Louis; de Koning, Harry P.; Caljon, Guy; Van Calenbergh, Serge. And the article was included in European Journal of Medicinal Chemistry on February 15,2020.Safety of 9-((2R,3R,5S)-3-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-9H-purin-6-ol The following contents are mentioned in the article:
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 therapeutic agents. T. brucei lacks the enzymes necessary to forge the purine ring from amino acid precursors, rendering them dependent on the uptake and interconversion of host purines. This dependency renders analogs of purines and corresponding nucleosides an interesting source of potential anti-T. brucei agents. In this study, we synthesized and evaluated a series of 7-substituted 7-deazainosine derivatives and found that 6-O-alkylated analogs in particular showed highly promising in vitro activity with EC50 values in the mid-nanomolar range. SAR investigation of the O-alkyl chain showed that antitrypanosomal activity increased, and also cytotoxicity, with alkyl chain length, at least in the linear alkyl chain series. However, this could be attenuated by introducing a terminal branch point, resulting in the highly potent and selective analogs,, e.g. I. No resistance related to transporter-mediated uptake could be identified, earmarking several of these analogs for further in vivo follow-up studies. This study involved multiple reactions and reactants, such as 9-((2R,3R,5S)-3-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-9H-purin-6-ol (cas: 13146-72-0Safety of 9-((2R,3R,5S)-3-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-9H-purin-6-ol).
9-((2R,3R,5S)-3-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-9H-purin-6-ol (cas: 13146-72-0) belongs to tetrahydrofuran derivatives. Solid acid catalysis, and the advantages often associated with their use, have been proved equally efficient for the synthesis of tetrahydrofurans or furans. THF (Tetrahydrofuran) is also used as a starting material for the synthesis of poly(tetramethylene ether) glycol (PTMG), etc.Safety of 9-((2R,3R,5S)-3-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-9H-purin-6-ol
13146-72-0;9-((2R,3R,5S)-3-Hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-9H-purin-6-ol;The future of 13146-72-0;New trend of C10H12N4O4 ;function of 13146-72-0