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Literature DB >> 10498218

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

C N Carrigan¹, C S Esslinger, R D Bartlett, R J Bridges, C M Thompson.

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.

Entities: Chemical Disease

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Year: 1999 PMID： 10498218 DOI： 10.1016/s0960-894x(99)00444-8

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

8 in total

1. Inhibition of vesicular glutamate uptake by Rose Bengal-related compounds: structure-activity relationship.

Authors: David G Bole; Tetsufumi Ueda
Journal: Neurochem Res Date: 2005-03 Impact factor: 3.996

2. Use of the hydantoin isostere to produce inhibitors showing selectivity toward the vesicular glutamate transporter versus the obligate exchange transporter system x(c)(-).

Authors: S Kaleem Ahmed; Jean-Louis G Etoga; Sarjubhai A Patel; Richard J Bridges; Charles M Thompson
Journal: Bioorg Med Chem Lett Date: 2011-05-14 Impact factor: 2.823

3. Conformationally-restricted amino acid analogues bearing a distal sulfonic acid show selective inhibition of system x(c)(-) over the vesicular glutamate transporter.

Authors: Jean-Louis G Etoga; S Kaleem Ahmed; Sarjubhai Patel; Richard J Bridges; Charles M Thompson
Journal: Bioorg Med Chem Lett Date: 2009-10-12 Impact factor: 2.823

4. The development of benzo- and naphtho-fused quinoline-2,4-dicarboxylic acids as vesicular glutamate transporter (VGLUT) inhibitors reveals a possible role for neuroactive steroids.

Authors: Christina N Carrigan; Sarjubhai A Patel; Holly D Cox; Erin S Bolstad; John M Gerdes; Wesley E Smith; Richard J Bridges; Charles M Thompson
Journal: Bioorg Med Chem Lett Date: 2013-12-25 Impact factor: 2.823

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

1. Inhibition of vesicular glutamate uptake by Rose Bengal-related compounds: structure-activity relationship.

2. Use of the hydantoin isostere to produce inhibitors showing selectivity toward the vesicular glutamate transporter versus the obligate exchange transporter system x(c)(-).

3. Conformationally-restricted amino acid analogues bearing a distal sulfonic acid show selective inhibition of system x(c)(-) over the vesicular glutamate transporter.

4. The development of benzo- and naphtho-fused quinoline-2,4-dicarboxylic acids as vesicular glutamate transporter (VGLUT) inhibitors reveals a possible role for neuroactive steroids.

5. Tetrapeptide inhibitors of the glutamate vesicular transporter (VGLUT).

Review 6. Are vesicular neurotransmitter transporters potential treatment targets for temporal lobe epilepsy?

7. Inhibition of the Vesicular Glutamate Transporter (VGLUT) with Congo Red Analogs: New Binding Insights.

Review 8. Molecular, Structural, Functional, and Pharmacological Sites for Vesicular Glutamate Transporter Regulation.