Use of the hydantoin isostere to produce inhibitors showing selectivity toward the vesicular glutamate transporter versus the obligate exchange transporter system
SK Ahmed, JLG Etoga, SA Patel, RJ Bridges…
Index: Ahmed, S. Kaleem; Etoga, Jean-Louis G.; Patel, Sarjubhai A.; Bridges, Richard J.; Thompson, Charles M. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 14 p. 4358 - 4362
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Citation Number: 9
Abstract
Abstract 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 View the MathML source
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