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

@article{Ahmed2011UseOT,
  title={Use of the hydantoin isostere to produce inhibitors showing selectivity toward the vesicular glutamate transporter versus the obligate exchange transporter system x(c)(-).},
  author={Sherifa K. Ahmed and Jean-Louis G Etoga and Sarjubhai Amratbhai Patel and Richard Bridges and Charles M. Thompson},
  journal={Bioorganic & medicinal chemistry letters},
  year={2011},
  volume={21 14},
  pages={4358-62}
}
Evidence was acquired prior to suggest that the vesicular glutamate transporter (VGLUT) but not other glutamate transporters were inhibited by structures containing a weakly basic α-amino group. To test this hypothesis, a series of analogs using a hydantoin (pK(a)∼9.1) isostere were synthesized and analyzed as inhibitors of VGLUT and the obligate cystine-glutamate transporter (system x(c)(-)). Of the hydantoin analogs tested, a thiophene-5-carboxaldehyde analog 2l and a bis-hydantoin 4b were… CONTINUE READING

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