Title of article :
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
Author/Authors :
Dean G. Brown، نويسنده , , Rebecca A. Urbanek، نويسنده , , Thomas M. Bare، نويسنده , , Frances M. McLaren، نويسنده , , Carey L. Horchler، نويسنده , , Megan Murphy، نويسنده , , Gary B. Steelman، نويسنده , , James R. Empfield، نويسنده , , Janet M. Forst، نويسنده , , Keith J. Herzog، نويسنده , , Wenhua Xiao، نويسنده , , Martin C. Dyroff، نويسنده , , Chi-Ming C. Lee، نويسنده , , Shephali Trivedi، نويسنده , , Kathy L. Neilson، نويسنده , , Richard A. Keith، نويسنده ,
Abstract :
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.
