Synthesis of 7-chloro-2,3-dihydro-2-[1-(pyridinyl)alkyl]-pyridazino[4,5- b ]quinoline-1,4,10(5 H )-triones as NMDA glycine-site antagonists
| Autor: | Dean G. Brown, Kathy L. Neilson, Horchler Carey, Thomas Michael Bare, Frances M. Mclaren, Gary Steelman, James Empfield, Richard A. Keith, Martin C. Dyroff, Wenhua Xiao, Rebecca Urbanek, Janet Marie Forst, Chi-Ming C. Lee, Shephali Trivedi, Keith John Herzog, Megan Murphy |
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| Rok vydání: | 2003 |
| Předmět: |
chemistry.chemical_classification
Stereochemistry Organic Chemistry Clinical Biochemistry Quinoline Glycine Substituent Pharmaceutical Science Receptors N-Methyl-D-Aspartate Biochemistry Chemical synthesis Pyridazines chemistry.chemical_compound chemistry Drug Discovery Quinolines Molecular Medicine NMDA receptor Solubility Molecular Biology Glycine receptor Alkyl |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 13:3553-3556 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(03)00750-9 |
| Popis: | Several members of the 7-chloro-2,3-dihydro-2-[1-(pyridinyl)alkyl]-pyridazino[4,5-b]quinoline-1,4,10(5H)-triones (2) have been identified as being potent and selective NMDA glycine-site antagonists. Increasing size of the alkyl substituent on the alpha-carbon led to a progressive decrease in binding affinity. Some of these analogues possess improved drug-like properties such as cellular permeability, solubility and oral absorption. |
| Databáze: | OpenAIRE |
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