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Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2015 Jul 17; Vol. 6 (8), pp. 861-5. Date of Electronic Publication: 2015 Jul 17 (Print Publication: 2015). - Publication Year :
- 2015
-
Abstract
- Hit-to-lead efforts resulted in the discovery of compound 19, a potent CYP11B2 inhibitor that displays high selectivity vs related CYPs, good pharmacokinetic properties in rat and rhesus, and lead-like physical properties. In a rhesus pharmacodynamic model, compound 19 displays robust, dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 6
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26288685
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.5b00048