Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists.

Basic Information

ID: ALA3352234

Journal: Bioorg Med Chem Lett

Title: Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists.

Authors: Hasegawa F, Niidome K, Migihashi C, Murata M, Negoro T, Matsumoto T, Kato K, Fujii A.

Abstract: Furan-2-carbohydrazides were found as orally active glucagon receptor antagonists. Starting from the hit compound 5, we successfully determined the structure activity relationships of a series of derivatives obtained by modifying the acidity of the phenol. We identified the ortho-nitrophenol as a good scaffold for glucagon receptor inhibitory activity. Our efforts have led to the discovery of compound 7l as a potent glucagon receptor antagonist with good bioavailability and satisfactory long half-life.

CiteXplore: 25127101

DOI: 10.1016/j.bmcl.2014.07.025

Patent ID: ┄