Quinoline-2,4-dicarboxylic acids: synthesis and evaluation as inhibitors of the glutamate vesicular transport system

Bioorg Med Chem Lett. 1999 Sep 6;9(17):2607-12. doi: 10.1016/s0960-894x(99)00444-8.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Biological Transport
  • Carrier Proteins / antagonists & inhibitors*
  • Carrier Proteins / metabolism
  • Dicarboxylic Acids / chemical synthesis*
  • Dicarboxylic Acids / pharmacology*
  • Evaluation Studies as Topic
  • Glutamic Acid / metabolism*

Substances

  • Carrier Proteins
  • Dicarboxylic Acids
  • Glutamic Acid