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

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. (C) 2003 Elsevier Ltd. All rights reserved.