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

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

ACS Med Chem Lett

Departments of Discovery Chemistry, Chemistry Modeling & Informatics, Hypertension, Drug Metabolism & Pharmacokinetics, and In Vitro Pharmacology, Merck Research Laboratories , Rahway, New Jersey 07065, United States.

Published: January 2017

AI Article Synopsis

  • Researchers discovered and optimized a series of spirocyclic piperidine compounds that inhibit aldosterone synthase (CYP11B2).
  • These inhibitors demonstrate strong potency in blocking CYP11B2 with good selectivity against similar enzymes.
  • The compounds also exhibit favorable physical and pharmacokinetic properties, making them promising candidates for further development.

Article Abstract

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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5238464PMC
http://dx.doi.org/10.1021/acsmedchemlett.6b00455DOI Listing

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