ORGN 545 |
| Keith R. Buszek, Paul W. Baures, and Om P. Malik. Department of Chemistry, Kansas State University, 111 Willard Hall, Manhattan, KS 66506-3701 |
| G-protein coupled receptors (GPCRs) form the largest class of expressed surface proteins and are arguably the most important protein class based on their role in the cell. There is growing evidence that GPCRs do not exist solely as monomeric proteins but may also form homodimers with another receptor of the same type and heterodimers with receptors of different subtypes or with receptors for different ligands. Bivalent ligands for GPCRs that link two bioactive compounds were first described over two decades ago with the reported example of an opioid bivalent ligand. However, there are very few reports of compounds that could be potential bivalent ligands for histamine receptors. This is surprising given the pharmacological importance of drugs targeting the histamine H1- and H2-receptors, as well as ongoing research in histamine H3-receptor design. In this presentation, we will describe our efforts to prepare a series of novel bivalent histamine receptor ligands that have various linker lengths, functionalities and orientations using combinations of urocanic acid, dihydrourocanic acid and imidazole-4-carboxylic acid with various diamines. |
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Bioorganic, Molecular Recognition, Asymmetric Reactions and Syntheses
11:00 AM-1:00 PM, Wednesday, September 10, 2003 Javits Convention Center -- Hall 1B/1C, Poster
Division of Organic Chemistry |