| Literature DB >> 11844695 |
Anthony Ling1, Michael Plewe, Javier Gonzalez, Peter Madsen, Christian K Sams, Jesper Lau, Vlad Gregor, Doug Murphy, Kimberly Teston, Atsuo Kuki, Shenghua Shi, Larry Truesdale, Dan Kiel, John May, James Lakis, Kenna Anderes, Eugenia Iatsimirskaia, Ulla G Sidelmann, Lotte B Knudsen, Christian L Brand, Alex Polinsky.
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.Entities:
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Year: 2002 PMID： 11844695 DOI： 10.1016/s0960-894x(01)00819-8
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823