anti-Nipah_081
| anti-Nipah_ID | anti-Nipah_081 |
| anti-Nipah Drug | 7-(4-carbamoylpiperidin-1-yl)-1-cyclopropyl-N-[(2,4-dichlorophenyl)methyl]-6-fluoro-4-oxo-1,2,3,4-tetrahydroquinoline-3-carboxamide |
| Nipah virus strain | NiV (Nipah G/F fusion expression vector) |
| Approaches used to test anti-Nipah activity | Experimental |
| Methods used to test anti-Nipah activity | in-vitro |
| Models used to test anti-Nipah activity | Vero |
| Mode of infection to test anti-Nipah activity | Transfection |
| Viral titer to test anti-Nipah activity | NA NA |
| Mode of Drug delivery for anti-Nipah activity | Culture |
| Time of Drug delivery for anti-Nipah activity | Post transfection |
| Duration of Drug delivery for anti-Nipah activity | 24 hours |
| Drug concentration used to test anti-Nipah activity | 1.5 μM |
| Assays used to test anti-Nipah activity | Syncytia formation |
| anti-Nipah activity | Decrease [Effective concentration (50 %)] |
| Cytotoxicity of anti-Nipah compounds | >20 _M |
| References | Niedermeier S, Singethan K, Rohrer SG, Matz M, Kossner M, Diederich S, Maisner A, Schmitz J, Hiltensperger G, Baumann K, Holzgrabe U, Schneider-Schaulies J. A small-molecule inhibitor of Nipah virus envelope protein-mediated membrane fusion. J Med Chem. 2009 Jul 23;52(14):4257-65. doi: 10.1021/jm900411s. |
| Comments | 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. |