Bioorganic and Medicinal Chemistry Letters p. 2849 - 2854 (1998)
Update date:2022-08-04
Topics:
Collado, Ivan
Ezquerra, Jesus
Mazon, Angel
Pedregal, Concepcion
Yruretagoyena, Belen
Kingston, Anne E.
Tomlinson, Rosemary
Wright, Rebecca A.
Johnson, Bryan G.
Schoepp, Darryle D.
2-(9-Xanthylmethyl)-2-(2'-carboxycyclopropyl) glycine 6e is a novel metabotropic glutamate receptor antagonist. A series of alpha, C-3' disubstituted (carboxycyclopropyl)glycines 6f-n were prepared. Antagonist activity was observed for all these compounds at group 2 and group 3 mGluRs. Although they were slightly less active on group 2 mGluRs than non C-3, substituted 6e, the compounds 6f-n were more selective with lesser or no activity on group 1 mGluR subtypes (IC50 values greater than 100μm).
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