Espadinha, Margarida published the artcileIdentification of tetracyclic lactams as NMDA receptor antagonists with potential application in neurological disorders, Category: catalysis-chemistry, the publication is European Journal of Medicinal Chemistry (2020), 112242, database is CAplus and MEDLINE.
The synthesis and pharmacol. evaluation of a new scaffold with antagonistic activity for NMDAR was reported. Specifically, a chem. library of eighteen 1-aminoindan-2-ol tetracyclic lactams was synthesized and screened as NMDAR antagonists. The compounds were obtained by chiral pool synthesis using enantiomerically pure 1-aminoindan-2-ols as chiral inductors, and their stereochem. was proven by X-ray crystallog. anal. of two target compounds Most compounds reveal NMDAR antagonism, and eleven compounds display IC50 values in a Ca2+ entry-sensitive fluo-4 assay in the same order of magnitude of memantine, a clin. approved NMDAR antagonist. Docking studies suggest that the novel compounds can act as NMDAR channel blockers since there is a compatible conformation with MK-801 co-crystallized with NMDAR channel. In addition, we show that the tetracyclic 1-aminoindan-2-ol derivatives are brain permeable and non-toxic, and we identify promising hits for further optimization as modulators of the NMDAR function.
European Journal of Medicinal Chemistry published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, Category: catalysis-chemistry.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia