Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists

Xiaojun Han; Sokhom S Pin; Kevin Burris; Lawrence K Fung; Stella Huang; Matthew T Taber; Jie Zhang; Gene M Dubowchik

doi:10.1016/j.bmcl.2005.06.028

Synthesis and structure-activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4029-32. doi: 10.1016/j.bmcl.2005.06.028.

Authors

Xiaojun Han¹, Sokhom S Pin, Kevin Burris, Lawrence K Fung, Stella Huang, Matthew T Taber, Jie Zhang, Gene M Dubowchik

Affiliation

¹ Pharmaceutical Research Institute, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA. xiaojun.han@bms.com

PMID: 15982881
DOI: 10.1016/j.bmcl.2005.06.028

Abstract

8-Aryl-1,3a,8-triaza-cyclopenta[a]indenes represent a novel series of high binding affinity corticotropin-releasing factor 1 receptor antagonists. Here, we report their synthesis, SAR, and pharmacokinetic properties of compound 8e (K(i) = 23 nM).

MeSH terms

Benzimidazoles / chemical synthesis
Benzimidazoles / chemistry*
Benzimidazoles / pharmacokinetics
Benzimidazoles / pharmacology*
Humans
Molecular Structure
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
Receptors, Corticotropin-Releasing Hormone / metabolism
Structure-Activity Relationship

Substances

Benzimidazoles
Receptors, Corticotropin-Releasing Hormone
CRF receptor type 1