《Identification of tetracyclic lactams as NMDA receptor antagonists with potential application in neurological disorders》 was written by Espadinha, Margarida; Viejo, Lucia; Lopes, Ricardo M. R. M.; Herrera-Arozamena, Clara; Molins, Elies; dos Santos, Daniel J. V. A.; Goncalves, Lidia; Rodriguez-Franco, Maria Isabel; de los Rios, Cristobal; Santos, Maria M. M.. Product Details of 126456-43-7 And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:
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. In the part of experimental materials, we found many familiar compounds, such as (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7Product Details of 126456-43-7)
(1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Product Details of 126456-43-7
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