Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy

  • Bioorg Med Chem Lett. 2005 Apr 15;15(8):2163-7. doi: 10.1016/j.bmcl.2005.02.009.
Christopher F Thompson  1 ,  Nazia Quraishi ,  Amjad Ali ,  James R Tata ,  Milton L Hammond ,  James M Balkovec ,  Monica Einstein ,  Lan Ge ,  Georgianna Harris ,  Theresa M Kelly ,  Paul Mazur ,  Shilpa Pandit ,  Joseph Santoro ,  Ayesha Sitlani ,  Chuanlin Wang ,  Joanne Williamson ,  Douglas K Miller ,  Ting-ting D Yamin ,  Chris M Thompson ,  Edward A O'Neill ,  Dennis Zaller ,  Michael J Forrest ,  Ester Carballo-Jane ,  Silvi Luell
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. [email protected]
PMID: 15808489 DOI: 10.1016/j.bmcl.2005.02.009
Abstract

A series of novel ligands for the Glucocorticoid Receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.