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Bioorg Med Chem Lett. 2005 Dec 1;15(23):5266-9. Epub 2005 Sep 26.

Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.

Author information

1
Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. xin_gu@merck.com

Abstract

Replacement of the pentyl chain on our original bicyclo[2.2.2]octyltriazole leads 1 and 2 has led to the discovery that heteroaryl substituted bicyclo[2.2.2]octyltriazoles are potent and selective 11beta-hydroxysteroid dehydrogenase type I (11beta-HSD1) inhibitors with excellent pharmacokinetic profiles.

PMID:
16185866
DOI:
10.1016/j.bmcl.2005.08.052
[Indexed for MEDLINE]

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