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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

✍ Scribed by Dean G. Brown; Rebecca A. Urbanek; Thomas M. Bare; Frances M. McLaren; Carey L. Horchler; Megan Murphy; Gary B. Steelman; James R. Empfield; Janet M. Forst; Keith J. Herzog; Wenhua Xiao; Martin C. Dyroff; Chi-Ming C. Lee; Shephali Trivedi; Kathy L. Neilson; Richard A. Keith

Book ID: 104364068
Publisher: Elsevier Science
Year: 2003
Tongue: English
Weight: 168 KB
Volume: 13
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(03)00750-9

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✦ Synopsis

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.

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