Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10590991 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
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.
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Authors
Futoshi Hasegawa, Kazumi Niidome, Chiaki Migihashi, Makoto Murata, Toshiyuki Negoro, Takafumi Matsumoto, Kaori Kato, Akihito Fujii,