| Autor: |
Daphne Szeto, Doris F. Cully, Scott B. Hoyt, Ning Ren, Elaine Tung, Charlene Bopp, Jack Gibson, Gino Salituro, Clare London, Jiaqiang Cai, Amjad Ali, Qing Chen, Andrea Sok, Simone Belshaw, Carrie Ann Maxwell, Mark Rosenbach, Gaochao Zhou, Gail Forrest, Tian-Quan Cai, Daniel R. McMasters, Lee-Yuh Pai, Nelo R. Rivera, Sloan Stribling, Emma Carswell, Richard Hajdu, Robinson John E, Andrew J. Cooke, Jeff Kuethe, Tom Wisniewski, Joe Metzger, Thomas R. Clarkson, Gui-Bai Liang, Mary Struthers, Jim Tata, Mike E. Lassman, Lindsay Brown, Wei Tang, Theresa McLaughlin, Xiuying Ma, Nicole Buist, Kun Liu, Joe Clemas, D. Jonathan Bennett, Andreas Verras, Min K. Park, Yusheng Xiong, John Maclean, Jose Castro-Perez |
| Jazyk: |
angličtina |
| Rok vydání: |
2015 |
| Předmět: |
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| Popis: |
We report the discovery of a benzimidazole series of CYP11B2 inhibitors. Hit-to-lead and lead optimization studies identified compounds such as 32, which displays potent CYP11B2 inhibition, high selectivity versus related CYP targets, and good pharmacokinetic properties in rat and rhesus. In a rhesus pharmacodynamic model, 32 produces dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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