Basic Information
ID: ALA1135077
Journal: Bioorg Med Chem Lett
Title: Human glucagon receptor antagonists based on alkylidene hydrazides.
Authors: Ling A, Plewe M, Gonzalez J, Madsen P, Sams CK, Lau J, Gregor V, Murphy D, Teston K, Kuki A, Shi S, Truesdale L, Kiel D, May J, Lakis J, Anderes K, Iatsimirskaia E, Sidelmann UG, Knudsen LB, Brand CL, Polinsky A.
Abstract: A series of alkylidene hydrazide derivatives containing an alkoxyaryl moiety was optimized. The resulting hydrazide-ethers were competitive antagonists at the human glucagon receptor. Pharmacokinetic experiments showed fast clearance of most of the compounds tested. A representative compound [4-hydroxy-3-cyanobenzoic acid (4-isopropylbenzyloxy-3,5-dimethoxymethylene)hydrazide] with an IC50 value of 20 nM was shown to reduce blood glucose levels in fasted rats.
CiteXplore: 11844695
DOI: 10.1016/s0960-894x(01)00819-8
Patent ID: ┄
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