Synthesis of 7-chloro-2,3-dihydro-2-[1-(pyridinyl)alkyl]-pyridazino[4,5-b]quinoline-1,4,10(5H)-triones as NMDA glycine-site antagonists |
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| Authors: | Brown Dean G Urbanek Rebecca A Bare Thomas M McLaren Frances M Horchler Carey L Murphy Megan Steelman Gary B Empfield James R Forst Janet M Herzog Keith J Xiao Wenhua Dyroff Martin C Lee Chi-Ming C Trivedi Shephali Neilson Kathy L Keith Richard A |
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| Institution: | AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE 19850, USA. dean.brown@astrazeneca.com |
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| Abstract: | Several members of the 7-chloro-2,3-dihydro-2-1-(pyridinyl)alkyl]-pyridazino4,5-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. |
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