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Bioorg Med Chem Lett. 2008 Jun 1;18(11):3412-6. doi: 10.1016/j.bmcl.2008.04.014. Epub 2008 Apr 10.

Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. yuping_zhu@merck.com

Abstract

3-(Phenylcyclobutyl)-1,2,4-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). These were active both in vitro and in an in vivo mouse pharmacodynamic (PD) model. Fluorine substitution of the cyclobutane ring improved the pharmacokinetic profile significantly. The synthesis and structure-activity relationships are presented.

PMID:
18440812
DOI:
10.1016/j.bmcl.2008.04.014
[Indexed for MEDLINE]

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