Discovery of Spirocyclic Aldosterone Synthase Inhibitors as Potential Treatments for Resistant Hypertension

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• 作者：Whitney L. PetrilliScott B. Hoyt ; Clare London ; Daniel McMasters ; Andreas Verras ; Mary Struthers ; Doris Cully ; Thomas Wisniewski ; Ning Ren ; Charlene Bopp ; Andrea Sok ; Qing Chen ; Ying Li ; Elaine Tung ; Wei Tang ; Gino Salituro ; Ian Knemeyer ; Bindhu Karanam ; Joseph Clemas ; Gaochao Zhou ; Jack Gibson ; Carrie Ann Shipley ; Douglas J. MacNeil ; Ruth Duffy ; James R. Tata ; Feroze Ujjainwalla ; Amjad Ali ; Yusheng Xiong
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：January 12, 2017
• 年：2017
• 卷：8
• 期：1
• 页码：128-132
• 全文大小：445K
• ISSN：1948-5875

文摘

Herein we report the discovery and hit-to-lead optimization of a series of spirocyclic piperidine aldosterone synthase (CYP11B2) inhibitors. Compounds from this series display potent CYP11B2 inhibition, good selectivity versus related CYP enzymes, and lead-like physical and pharmacokinetic properties.