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Bioorg Med Chem Lett. 2005 Jun 2;15(11):2752-7.

Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.

Author information

1
Metabolic Disease Research, Abbott Laboratories, Abbott Park, IL 60064, USA. andrew.souers@abbott.com

Abstract

A series of urea-based N-1-(2-aminoethyl)-indazoles was synthesized and evaluated for melanin-concentrating hormone receptor 1 (MCHr1) antagonism in both binding and functional assays. Several compounds that acted as MCHr1 antagonists were identified, and optimization afforded a compound with excellent binding affinity, good functional potency, and oral efficacy in a chronic model for weight loss in diet-induced obese mice.

PMID:
15911251
DOI:
10.1016/j.bmcl.2005.03.114
[Indexed for MEDLINE]

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