The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-Beta-hydroxylase
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Adams, Christopher, Hu, Chii-Whei, Jeng, Arco, Karki, Rajeshri, Ksander, Gary, Lasala, Daniel, Leung-Chu, Jennifer, Liang, Guiqing, Liu, Qian, Meredith, Erik, Rao, Chang, Rigel, Dean, Springer, Clayton, Zhang, Chun, Shi, Jie and Smith, Sherri (2010) The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-Beta-hydroxylase. Bioorganic and Medicinal Chemistry Letters, 20 (15). pp. 4324-4327.
Abstract
Aldosterone, the final component of the renin-angiotensin-aldosterone system, plays an important role in the pathophysiology of hypertension and congestive heart failure. Aldosterone synthase (CYP11B2) catalyzes the last three steps of aldosterone biosynthesis, and as such appears to be a target for the treatment of these disorders. A sulfonamide-imidazole scaffold has proven to be a potent inhibitor of CYP11B2. Furthermore, this scaffold can achieve high levels of selectivity for CYP11B2 over CYP11B1, a key enzyme in the biosynthesis of cortisol.
| Item Type: | Article |
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| Additional Information: | A list of the structures disclosed in this manuscript has been sent out to the GDC Leadership team. There were no objections. |
| Keywords: | Aldosterone, Aldosterone Synthase, CYP11B2, CYP11B1, hypertension |
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| Date Deposited: | 13 Oct 2015 13:16 |
| Last Modified: | 13 Oct 2015 13:16 |
| URI: | https://oak.novartis.com/id/eprint/2598 |