Surivet, Jean-Philippe; Zumbrunn, Cornelia; Rueedi, Georg; Hubschwerlen, Christian; Bur, Daniel; Bruyere, Thierry; Locher, Hans; Ritz, Daniel; Keck, Wolfgang; Seiler, Peter; Kohl, Christopher; Gauvin, Jean-Christophe; Mirre, Azely; Kaegi, Verena; Dos Santos, Marina; Gaertner, Mika; Delers, Jonathan; Enderlin-Paput, Michel; Boehme, Maria published the article 《Design, Synthesis, and Characterization of Novel Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Potent Anti-Gram-Positive Activity》. Keywords: pyran tetrahydro Gram pos bacterial topoisomerase inhibitor; DNA gyrase topoisomerase inhibitor tetrahydropyran bicyclic aromatic derivative.They researched the compound: tert-Butyl ((3R,6S)-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)carbamate( cas:603130-12-7 ).Computed Properties of C11H21NO4. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:603130-12-7) here.
There is an urgent need for new antibacterial drugs that are effective against infections caused by multidrug-resistant pathogens. Novel nonfluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) have the potential to become such drugs because they display potent antibacterial activity and exhibit no target-mediated cross-resistance with fluoroquinolones. Bacterial topoisomerase inhibitors that are built on a tetrahydropyran ring linked to a bicyclic aromatic moiety through a syn-diol linker show potent anti-Gram-pos. activity, covering isolates with clin. relevant resistance phenotypes. For instance, analog I was found to be a dual DNA gyrase-topoisomerase IV inhibitor, with broad antibacterial activity and low propensity for spontaneous resistance development, but suffered from high hERG K+ channel block. On the other hand, analog II displayed lower hERG K+ channel block while retaining potent in vitro antibacterial activity and acceptable frequency for resistance development. Furthermore, analog II showed moderate clearance in rat and promising in vivo efficacy against Staphylococcus aureus in a murine infection model.
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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics