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Bioorg Med Chem. 2007 Mar 1;15(5):2054-80. Epub 2006 Dec 23.

Azetidinones as vasopressin V1a antagonists.

Author information

1
Department of Chemistry, 6 East Packer Avenue, Lehigh University, Bethlehem, PA 18015, USA. chg3@lehigh.edu

Abstract

The azetidinone LY307174 (1) was identified as a screening lead for the vasopressin V1a receptor (IC50 45 nM at the human V1a receptor) based on molecular similarity to ketoconazole (2), a known antagonist of the luteinizing hormone releasing hormone receptor. Structure-activity relationships for the series were explored to optimize receptor affinity and pharmacokinetic properties, resulting in compounds with Ki values <1nM and brain levels after oral dosing approximately 100-fold higher than receptor affinities.

PMID:
17234419
PMCID:
PMC2067992
DOI:
10.1016/j.bmc.2006.12.031
[Indexed for MEDLINE]
Free PMC Article

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