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Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp³)-H Activation Strategy and Structure-Activity Relationship Studies at the Ionotropic Glutamate Receptors.

ABSTRACT: Competitive antagonists for ionotropic glutamate receptors (iGluRs) are highly valuable tool compounds for studying health and disease states in the central nervous system. However, only few subtype selective tool compounds are available and the discovery of antagonists with novel iGluR subtype selectivity profiles remains a profound challenge. In this paper, we report an elaborate structure-activity relationship (SAR) study of the parental scaffold 2,3-trans-3-carboxy-3-phenyl-proline by the synthesis of 40 new analogues. Three synthetic strategies were employed with two new strategies of which one being a highly efficient and fully enantioselective strategy based on C(sp3)-H activation methodology. The SAR study led to the conclusion that selectivity for the NMDA receptors was a g

SUBMITTER: Kayser S

PROVIDER: S-EPMC7227796 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature

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Dataset Information

Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp³)-H Activation Strategy and Structure-Activity Relationship Studies at the Ionotropic Glutamate Receptors.

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Dataset Information

Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp3)-H Activation Strategy and Structure-Activity Relationship Studies at the Ionotropic Glutamate Receptors.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp³)-H Activation Strategy and Structure-Activity Relationship Studies at the Ionotropic Glutamate Receptors.