Mueller, Sebastian L.’s team published research in European Journal of Medicinal Chemistry in 129 | CAS: 636-73-7

European Journal of Medicinal Chemistry published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, COA of Formula: C5H5NO3S.

Mueller, Sebastian L. published the artcileSystematic variation of the benzenesulfonamide part of the GluN2A selective NMDA receptor antagonist TCN-201, COA of Formula: C5H5NO3S, the publication is European Journal of Medicinal Chemistry (2017), 124-134, database is CAplus and MEDLINE.

GluN2A subunit containing N-methyl-D-aspartate receptors (NMDARs) are highly involved in various physiol. 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 pathol. processes is not exactly elucidated. In order to obtain potent and selective inhibitors of GluN2A subunit containing NMDARs, the selective neg. 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

European Journal of Medicinal Chemistry published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, COA of Formula: C5H5NO3S.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem