Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2005 Oct 15;15(20):4564-9.

Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.

Author information

1
Department of Basic Chemistry, Merck Research Laboratories, PO Box 2000, RY50G-146, Rahway, NJ 07065, USA. dongming_shen@merck.com

Abstract

A novel class of spiro-ureas has been discovered as potent human glucagon receptor antagonists in both binding and functional assays. Preliminary studies have revealed that compound 15 is an orally active human glucagon receptor antagonist in a transgenic murine pharmacodynamic model at 10 and 30 mpk. Compound 15 is orally bioavailable in several preclinical species and shows selectivity toward cardiac ion channels and other family B receptors, such as hGIP1 and hGLP.

PMID:
16102966
DOI:
10.1016/j.bmcl.2005.06.101
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center