|
|||||
|
|
Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist |
|
| Authors: | Nicholas P. Barton Benjamin R. Bellenie Andrew T. Doran Amanda J. Emmons Jag P. Heer Cristian M. Salvagno |
| Affiliation: | 1. GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park (North), Coldharbour Road, Harlow, Essex CM19 5AD, England, UK;2. GlaxoSmithKline S.p.A., Medicines Research Centre, Via Fleming 2, Verona, Italy |
| Abstract: | The optimisation of a tertiary sulfonamide high-throughput screening hit is described. A combination of high-throughput chemistry, pharmacophore analysis and in silico PK profiling resulted in the discovery of potent sulfonamide oxytocin receptor antagonists with oral exposure and good selectivity over vasopressin receptors. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |