Abstract
Exploiting the SAR of the known pyrrole derivatives, a new class of mGluR1 antagonists was developed through a cyclization of the C-2 position on the pyrrole N-1 nitrogen. The resulting pyrrolo[1,2-a]pyrazinones are potent and noncompetitive antagonists.
MeSH terms
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Animals
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CHO Cells
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Cricetinae
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Inhibitory Concentration 50
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Molecular Structure
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Pyrazines / chemistry*
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Pyrazines / pharmacology*
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Pyrroles / chemistry*
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Receptors, Metabotropic Glutamate / antagonists & inhibitors*
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Receptors, Metabotropic Glutamate / metabolism
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Structure-Activity Relationship
Substances
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Pyrazines
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Pyrroles
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor type 1