Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2009 Jul 1;19(13):3682-5. doi: 10.1016/j.bmcl.2009.02.123. Epub 2009 Mar 5.

Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold.

Author information

1
Merck-Serono, 4 Avenue du Président Mitterrand, 91380 Chilly-Mazarin, France.

Abstract

Spiro-carboxamides were identified as inhibitors of 11beta-hydroxysteroid-dehydrogenase type 1 by high-throughput screening. Structure-based drug design was used to optimise the initial hit yielding a sub-nanomolar IC(50) inhibitor (0.5nM) on human 11beta-HSD1 with a high binding efficiency index (BEI of 32.7) which was selective against human 11beta-HSD2 (selectivity ratio>200000).

PMID:
19450980
DOI:
10.1016/j.bmcl.2009.02.123
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center