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Synthesis and Biological Evaluation of Novel N-substituted Nipecotic Acid Derivatives With a Trans-Alkene Spacer as Potent GABA Uptake Inhibitors

Synthesis and Biological Evaluation of Novel N-substituted Nipecotic Acid Derivatives With a Trans-Alkene Spacer as Potent GABA Uptake Inhibitors

Krisztián Tóth, Georg Höfner, Klaus T Wanner

Bioorg Med Chem. 2018 Dec 1;26(22):5944-5961.

PMID: 30442505

Abstract:

Our study presents the synthesis and structure-activity relationship (SAR) of novel N-substituted nipecotic acid derivatives closely related to DDPM-1457 [(S)-2a], a chemically stable analog of (S)-SNAP-5114 (1), in the pursuit of finding new and potent mGAT4 selective inhibitors. Iminium ion chemistry served as key step for the preparation of the desired, new N-substituted nipecotic acid derivatives containing a variety of different heterocycles attached to the nipecotic acid moiety via a trans-alkene spacer. The target compounds were characterized with regard to their potency at and subtype selectivity for the GABA transporters mGAT1-mGAT4.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP157604552	(S)-SNAP-5114		157604-55-2	Price

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