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

CN Carrigan, CS Esslinger, RD Bartlett…

文献索引:Carrigan, Christina N.; Esslinger, C. Sean; Bartlett, Richard D.; Bridges, Richard J.; Thompson, Charles M. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 17 p. 2607 - 2612

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被引用次数: 29

摘要

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.