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Synthesis and Biological Evaluation of Novel N-substituted Nipecotic Acid Derivatives With an Alkyne Spacer as GABA Uptake Inhibitors

Synthesis and Biological Evaluation of Novel N-substituted Nipecotic Acid Derivatives With an Alkyne Spacer as GABA Uptake Inhibitors

Krisztián Tóth, Georg Höfner, Klaus T Wanner

Bioorg Med Chem. 2018 Jul 23;26(12):3668-3687.

PMID: 29886082

Abstract:

In this study, we present the synthesis and structure-activity relationships (SAR) of novel N-substituted nipecotic acid derivatives closely related to (S)-SNAP-5114 (2) in the pursuit of finding new and potent mGAT4 selective inhibitors. By the use of iminium ion chemistry, a series of new N-substituted nipecotic acid derivatives containing a variety of heterocycles, and an alkyne spacer were synthesized. Biological evaluation of the prepared compounds showed, how the inhibitory potency and subtype selectivity for the murine GABA transporters (mGATs) were influenced by the performed modifications.

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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