Abstract
We described the synthesis and biological evaluation of MPEP analogs functionalized at the position 3 of the phenyl ring. The results point out the limitation in the choice of a functional group at this position; the only substituents leading to retention of activity are NO(2) (IC(50)=13 nM) and CN (IC(50)=8 nM).
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Inhibitory Concentration 50
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Mice
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Receptors, Kainic Acid / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Gluk1 kainate receptor
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Pyridines
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Receptors, Kainic Acid
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6-methyl-2-(phenylethynyl)pyridine