82657-76-9Relevant academic research and scientific papers
Lifitegrast intermediate and preparation method thereof
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, (2021/07/08)
The invention relates to the field of pharmaceutical and chemical production, and discloses a lifitegrast intermediate and a preparation method thereof. A reaction route of the preparation method is as described in the specification. The preparation metho
Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues
Wang, Shuang-Yan,Larsen, Younes,Navarrete, Cristina Vara,Jensen, Anders A.,Nielsen, Birgitte,Al-Musaed, Ali,Frydenvang, Karla,Kastrup, Jette Sandholm,Pickering, Darryl S.,Clausen, Rasmus Pr?torius
, p. 2244 - 2254 (2016/03/25)
A series of analogues of the (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) receptor agonist BnTetAMPA (5b) were synthesized and characterized pharmacologically in radioligand binding assays at native and cloned AMPA receptors and functionally by two-electrode voltage clamp electrophysiology at the four homomeric AMPA receptors expressed in Xenopus laevis oocytes. The analogues 6 and 7 exhibit very different pharmacological profiles with binding affinity preference for the subtypes GluA1 and GluA3, respectively. X-ray crystal structures of three ligands (6, 7, and 8) in complex with the agonist binding domain (ABD) of GluA2 show that they induce full domain closure despite their low agonist efficacies. Trp767 in GluA2 ABD could be an important determinant for partial agonism of this compound series at AMPA receptors, since agonist efficacy also correlated with the location of the Trp767 side chain.
Sulphone-substituted quinazoline derivatives as immuno-modulators, their preparation and use as medicaments
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Page/Page column 11, (2011/07/29)
The present invention relates to sulphone-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various diseases.
