169616-29-9Relevant academic research and scientific papers
Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones
Jeannot, Frédéric,Taillier, Thomas,Despeyroux, Pierre,Renard, Stéphane,Rey, Astrid,Mourez, Micha?l,Poeverlein, Christoph,Khichane, Imène,Perrin, Marc-Antoine,Versluys, Stéphanie,Stavenger, Robert A.,Huang, Jianzhong,Germe, Thomas,Maxwell, Anthony,Cao, Sha,Huseby, Douglas L.,Hughes, Diarmaid,Bacqué, Eric
, p. 3565 - 3581 (2018)
In our quest for new antibiotics able to address the growing threat of multidrug resistant infections caused by Gram-negative bacteria, we have investigated an unprecedented series of non-quinolone bacterial topoisomerase inhibitors from the Sanofi patrim
Discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1
Jadhav, Gopal P.,Kaur, Ishwinder,Maryati, Maryati,Airhihen, Blessing,Fischer, Peter M.,Winkler, G. Sebastiaan
, p. 4219 - 4224 (2015)
Eukaryotic mRNA contains a 3′ poly(A) tail, which plays important roles in the regulation of mRNA stability and translation. Well-characterized enzymes involved in the shortening of the poly(A) tail include the multi-subunit Ccr4-Not deadenylase, which contains the Caf1 (Pop2) and Ccr4 catalytic components, and poly(A)-specific ribonuclease (PARN). Two Mg2+ ions present in the active sites of these ribonucleases are required for RNA cleavage. Here, we report the discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as (sub)micromolar inhibitors of Caf1.
1-Substituted xanthines
Bridson,Wang
, p. 855 - 858 (2007/10/02)
A convenient general procedure for the preparation of 1-alkyl-, 1-aryl-, and 1-aminoxanthines from an easily prepared imidazole precursor is described.
