α-Substituted quisqualic acid analogs: New metabotropic glutamate receptor group II selective antagonists

Alan P. Kozikowski; Darryl Steensma; Mario Varasi; Sergey Pshenichkin; Elena Surina; Jarda T. Wroblewski

doi:10.1016/S0960-894X(98)00052-3

α-Substituted quisqualic acid analogs: New metabotropic glutamate receptor group II selective antagonists

Alan P. Kozikowski, Darryl Steensma, Mario Varasi, Sergey Pshenichkin, Elena Surina, Jarda T. Wroblewski

School of Medicine

Research output: Contribution to journal › Article › peer-review

Abstract

Syntheses of both the α-methyl and benzyl analogs of quisqualic acid are described. Testing of these compounds for their activity at excitatory amino acid receptors revealed a striking change in activity in comparison to quisqualic acid. This structural modification results in the loss of quisqualate's potent agonist action at both non-NMDA ionotropic glutamate receptors as well as at group I mGluRs, while allowing these analogs to acquire antagonist properties with relative selectivity for group II metabotropic glutamate receptors.

Original language	English (US)
Pages (from-to)	447-452
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	8
Issue number	5
DOIs	https://doi.org/10.1016/S0960-894X(98)00052-3
State	Published - Mar 3 1998

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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α-Substituted quisqualic acid analogs : New metabotropic glutamate receptor group II selective antagonists. / Kozikowski, Alan P.; Steensma, Darryl; Varasi, Mario; Pshenichkin, Sergey; Surina, Elena; Wroblewski, Jarda T.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 8, No. 5, 03.03.1998, p. 447-452.

Research output: Contribution to journal › Article › peer-review

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