TY - DATA T1 - 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 PY - 2016/04/27 AU - Zanda Bluke AU - Einars Paass AU - Meik Sladek AU - Ulrich Abel AU - Valerjans Kauss UR - https://tandf.figshare.com/articles/journal_contribution/Synthesis_of_3_4_dihydro_2_i_H_i_1_2_benzothiazine_3_carboxylic_acid_1_1_dioxides_and_their_evaluation_as_ligands_for_NMDA_receptor_glycine_binding_site/3203584 DO - 10.6084/m9.figshare.3203584.v1 L4 - https://ndownloader.figshare.com/files/5028475 KW - NMDA receptor glycine binding site KW - benzothiazine KW - acid KW - membrane preparations KW - NH group KW - NMDA receptor ligands KW - -3-carboxylic KW - dioxide KW - glycine binding site KW - sp 3 CH 2 KW - NMDA receptor KW - 2- arylcarbonylmethyl KW - binding affinity KW - -2 KW - dihydro N2 - 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 [3H]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 sp3 CH2 is tolerated. This finding may pave the way for previously unexplored approaches for designing new ligands of the NMDA receptor. ER -