Probing the steric space at the floor of the D1 dopamine receptor orthosteric binding domain: 7α-, 7β-, 8α-, and 8β-methyl substituted dihydrexidine analogues

…, A Gallardo-Godoy, JI Juncosa Jr, PA Vidi…

文献索引：Cueva, Juan Pablo; Gallardo-Godoy, Alejandra; Juncosa, Jose I.; Vidi, Pierre A.; Lill, Markus A.; Watts, Val J.; Nichols, David E. Journal of Medicinal Chemistry, 2011 , vol. 54, # 15 p. 5508 - 5521

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被引用次数: 5

摘要

To probe the space at the floor of the orthosteric ligand binding site in the dopamine D1 receptor, four methylated analogues of dihydrexidine (DHX) were synthesized with substitutions at the 7 and 8 positions. The 8α-axial, 8β-equatorial, and 7α-equatorial were synthesized by photochemical cyclization of appropriately substituted N-benzoyl enamines, and the 7β-axial analogue was prepared by an intramolecular Henry reaction. All of the ...