218964-99-9Relevant academic research and scientific papers
Synthesis and evaluation of a novel series of phosphodiesterase IV inhibitors. A potential treatment for asthma
Beasley, Steven C.,Cooper, Nicola,Gowers, Lewis,Gregory, Joanna P.,Haughan, Alan F.,Hellewell, Paul G.,Macari, David,Miotla, Jadwiga,Montana, John G.,Morgan, Trevor,Naylor, Robert,Runcie, Karen A.,Tuladhar, Bishwa,Warneck, Julie B. H.
, p. 2629 - 2634 (1998)
The synthesis and pharmacological profile of a novel series of potent and selective phosphodiesterase type IV (PDE IV) inhibitors is described.
A small-molecule inhibitor of nipah virus envelope protein-mediated membrane fusion
Niedermeier, Sabine,Singethan, Katrin,Rohrer, Sebastian G.,Matz, Magnus,Kossner, Markus,Diederich, Sandra,Maisner, Andrea,Schmitz, Jens,Hiltensperger, Georg,Baumann, Knut,Holzgrabe, Ulrike,Schneider-Schaulies, Jurgen
supporting information; experimental part, p. 4257 - 4265 (2010/03/04)
Nipah virus (NiV), a highly pathogenic paramyxovirus, causes respiratory disease in pigs and severe febrile encephalitis in humans with high mortality rates. On the basis of the structural similarity of viral fusion (F) proteins within the family Paramyxoviridae, we designed and tested 18 quinolone derivatives in a NiV and measles virus (MV) envelope protein-based fusion assay beside evaluation of cytotoxicity. We found five compounds successfully inhibiting NiV envelope protein-induced cell fusion. The most active molecules (19 and 20), which also inhibit the syncytium formation induced by infectious NiV and show a low cytotoxicity in Vero cells, represent a promising lead quinolone-type compound structure. Molecular modeling indicated that compound 19 fits well into a particular protein cavity present on the NiV F protein that is important for the fusion process. 2009 American Chemical Society.
