| Literature DB >> 11543683 |
A Ling1, Y Hong, J Gonzalez, V Gregor, A Polinsky, A Kuki, S Shi, K Teston, D Murphy, J Porter, D Kiel, J Lakis, K Anderes, J May, L B Knudsen, J Lau.
Abstract
High throughput screening of our small molecule combinatorial library identified a class of benzoylnaphthalenehydrazones with modest affinity for the human glucagon receptor. Optimization of this initial hit through a series of targeted libraries and traditional medicinal chemistry led to ligands with nanomolar affinities. Pharmacological evaluation demonstrated that these ligands were competitive glucagon receptor antagonists. Intravenous administration of a representative benzoylnaphthalenehydrazone into rats attenuated glucagon-stimulated glucose levels.Entities:
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Year: 2001 PMID： 11543683 DOI： 10.1021/jm000547o
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446