1413281-77-2Relevant academic research and scientific papers
2 -AMINO- 1, 8 -NAPHTHYRIDINE-3 -CARBOXAMIDE DERIVATIVES AS ANTIMICROBIAL AGENTS
-
Page/Page column 60, (2013/06/05)
The present invention concerns novel 2-amino-1,8-naphthyridine-3-carboxamide derivatives of formula I, a pharmaceutical antibacterial composition containing them and the use of these compounds in the manufacture of a medicament for the treatment of infect
Structure-guided design, synthesis and biological evaluation of novel DNA ligase inhibitors with in vitro and in vivo anti-staphylococcal activity
Surivet, Jean-Philippe,Lange, Roland,Hubschwerlen, Christian,Keck, Wolfgang,Specklin, Jean-Luc,Ritz, Daniel,Bur, Daniel,Locher, Hans,Seiler, Peter,Strasser, Daniel Stefan,Prade, Lars,Kohl, Christopher,Schmitt, Christine,Chapoux, Ga?lle,Ilhan, Eser,Ekambaram, Nadia,Athanasiou, Alcibiade,Knezevic, Andreja,Sabato, Daniela,Chambovey, Alain,Gaertner, Mika,Enderlin, Michel,Boehme, Maria,Sippel, Virginie,Wyss, Pierre
, p. 6705 - 6711 (2013/01/14)
A series of 2-amino-[1,8]-naphthyridine-3-carboxamides (ANCs) with potent inhibition of bacterial NAD+-dependent DNA ligases (LigAs) evolved from a 2,4-diaminopteridine derivative discovered by HTS. The design was guided by several highly resolved X-ray structures of our inhibitors in complex with either Streptococcus pneumoniae or Escherichia coli LigA. The structure-activity-relationship based on the ANC scaffold is discussed. The in-depth characterization of 2-amino-6-bromo-7-(trifluoromethyl)-[1,8]- naphthyridine-3-carboxamide, which displayed promising in vitro (MIC Staphylococcus aureus 1 mg/L) and in vivo anti-staphylococcal activity, is presented.
