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The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-Beta-hydroxylase

Adams, Christopher and Hu, Chii-Whei and Jeng, Arco and Karki, Rajeshri and Ksander, Gary and Lasala, Daniel and Leung-Chu, Jennifer and Liang, Guiqing and Liu, Qian and Meredith, Erik and Rao, Chang and Rigel, Dean and Springer, Clayton and Zhang, Chun and 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

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