2. Academic Validation
  3. An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist

An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist

  • Bioorg Med Chem Lett. 2003 Jul 21;13(14):2307-10. doi: 10.1016/s0960-894x(03)00431-1.
Bryan K Sorensen 1,  J T Link,  Thomas von Geldern,  Maurice Emery,  Jiahong Wang,  Bach Hickman,  Marlena Grynfarb,  Annika Goos-Nilsson,  Sherry Carroll
Affiliations

Affiliation

  • 1 Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, 60064, Abbott Park, IL, USA. bryan.k.sorensen@abbott.com
PMID: 12824023 DOI: 10.1016/s0960-894x(03)00431-1
Abstract

A beta-C-glucuronide conjugate of the Glucocorticoid Receptor antagonist, Mifepristone 1, was prepared which maintained binding affinity, had modest in vitro activity, and was metabolically more stable than the parent. Pharmacokinetic studies suggest that the conjugate is recognized by the liver like O-glucuronides and may undergo a portion of the enterohepatic recirculation loop.

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