690646-06-1Relevant academic research and scientific papers
Systematic variation of the benzoylhydrazine moiety of the GluN2A selective NMDA receptor antagonist TCN-201
Schreiber, Julian A.,Müller, Sebastian L.,Westph?linger, Stefanie E.,Schepmann, Dirk,Strutz-Seebohm, Nathalie,Seebohm, Guiscard,Wünsch, Bernhard
supporting information, p. 259 - 269 (2018/09/18)
GluN2A containing N-methyl-D-aspartate receptors (NMDARs) are important ion channels in the central nervous system and highly involved in several different neurophysiological but also neuropathophysiological processes. However, current understanding of th
Systematic variation of the benzenesulfonamide part of the GluN2A selective NMDA receptor antagonist TCN-201
Müller, Sebastian L.,Schreiber, Julian A.,Schepmann, Dirk,Strutz-Seebohm, Nathalie,Seebohm, Guiscard,Wünsch, Bernhard
supporting information, p. 124 - 134 (2017/02/23)
GluN2A subunit containing N-methyl-D-aspartate receptors (NMDARs) are highly involved in various physiological processes in the central nervous system, but also in some diseases, such as anxiety, depression and schizophrenia. However, the role of GluN2A subunit containing NMDARs in pathological processes is not exactly elucidated. In order to obtain potent and selective inhibitors of GluN2A subunit containing NMDARs, the selective negative allosteric modulator 2 was systematically modified at the benzenesulfonamide part. The activity of the test compounds was recorded in two electrode voltage clamp experiments using Xenopus laevis oocytes expressing exclusively NMDARs with GluN1a and GluN2A subunits. It was found that halogen atoms in 3-position of the benzenesulfonamide part result in high GluN2A antagonistic activity. With an IC50 value of 204?nM the 3-bromo derivative 5i (N-{4-[(2-benzoylhydrazino)carbonyl]benzyl}-3-bromobenzenesulfonamide) has 2.5-fold higher antagonistic activity than the lead compound 2 and represents our new lead compound.
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice
Zhang, Xu,Zhou, Zhou,Yang, Huaiyu,Chen, Junhua,Feng, Ying,Du, Lili,Leng, Ying,Shen, Jianhua
supporting information; experimental part, p. 4455 - 4458 (2010/04/05)
Selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have considerable potential as treatments for type 2 diabetes. Presented herein are the syntheses, structure-activity relationships, and efficacy evaluation of 4-(phenylsulfonamido
