Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties

…, C Valcarce-Aspegren, M Guldbrandt…

文献索引：Madsen, Peter; Kodra, Janos T.; Behrens, Carsten; Nishimura, Erica; Jeppesen, Claus B.; Pridal, Lone; Andersen, Birgitte; Knudsen, Lotte B.; Valcarce-Aspegren, Carmen; Guldbrandt, Mette; Christensen, Inge T.; Jorgensen, Anker S.; Ynddal, Lars; Brand, Christian L.; Bagger, Morten Aa.; Lau, Jesper Journal of Medicinal Chemistry, 2009 , vol. 52, # 9 p. 2989 - 3000

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被引用次数: 25

摘要

The aim of the work presented here was to design and synthesize potent human glucagon receptor antagonists with improved pharmacokinetic (PK) properties for development of pharmaceuticals for the treatment of type 2 diabetes. We describe the preparation of compounds with cyclic cores (5-aminothiazoles), their binding affinities for the human glucagon and GIP receptors, as well as affinities for rat, mouse, pig, dog, and monkey ...