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Synthesis of 3,4-dihydro-2H-1,2-benzothiazine-3-carboxylic Acid 1,1-dioxides and Their Evaluation as Ligands for NMDA Receptor Glycine Binding Site

Synthesis of 3,4-dihydro-2H-1,2-benzothiazine-3-carboxylic Acid 1,1-dioxides and Their Evaluation as Ligands for NMDA Receptor Glycine Binding Site

Zanda Bluke, Einars Paass, Meik Sladek, Ulrich Abel, Valerjans Kauss

J Enzyme Inhib Med Chem. 2016 Aug;31(4):664-73.

PMID: 26114309

Abstract:

A series of 2-substituted 3,4-dihydro-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxides were synthesized and evaluated for their affinity to the glycine binding site of the N-methyl-d-aspartate (NMDA) receptor. The binding affinity was determined by the displacement of radioligand [(3)H]MDL-105,519 from rat cortical membrane preparations. The most attractive structures in the search for prospective NMDA receptor ligands were identified to be 2-arylcarbonylmethyl substituted 3,4-dihydro-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxides. It has been demonstrated for the first time that the replacement of NH group in the ligand by sp(3) CH2 is tolerated. This finding may pave the way for previously unexplored approaches for designing new ligands of the NMDA receptor.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
LS7931276	3,4-Dihydro-2H-1,5-benzodioxepin-7-ylboronic acid			Price

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