Quinoline-2,4-dicarboxylic acids: synthesis and evaluation as inhibitors of the glutamate vesicular transport system.
Twenty-six quinoline-2,4-dicarboxylic acids (QDC's) were synthesized by a modified Doebner-von Miller pathway and tested as inhibitors against the glutamate vesicular transport (GVT) protein. The QDC's were active as inhibitors with the most potent QDC's found to contain halogens at the 6-/8-position, a hydroxyl at the 8-position, or a tethered aromatic moiety at the 6- or 7-position of the quinoline.
Carrigan
C N
CN
Department of Pharmaceutical Sciences, The University of Montana, Missoula 59812, USA.
Esslinger
C S
CS
Bartlett
R D
RD
Bridges
R J
RJ
Thompson
C M
CM
D001692:Biological Transport; D002352:Carrier Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D003998:Dicarboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D005069:Evaluation Studies as Topic; D018698:Glutamic Acid / Q000378:metabolism*
D002352:Carrier Proteins; D003998:Dicarboxylic Acids; D018698:Glutamic Acid