Synthesis and biological evaluation of 6-aryl-6H-pyrrolo [3, 4-d] pyridazine derivatives: high-affinity ligands to the α 2 δ subunit of voltage gated calcium channels

…, BT Campbell, C Chen, M Cramer, T Hu, X Jiang…

文献索引：Stearns, Brian A.; Anker, Naomi; Arruda, Jeannie M.; Campbell, Brian T.; Chen, Chixu; Cramer, Merryl; Hu, Tao; Jiang, Xiaohui; Park, Kenneth; Ren, Kun Kun; Sablad, Marciano; Santini, Angelina; Schaffhauser, Herve; Urban, Mark O.; Munoz, Benito Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 5 p. 1295 - 1298

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被引用次数: 16

摘要

A novel class of 6-aryl-6H-pyrrolo [3, 4-d] pyridazine ligands for the α2δ subunit of voltage- gated calcium channels has been described. Substitutions in the aryl ring of the molecule were generally not tolerated, and resulted in diminished binding to the α2δ subunit. Modifications to the pyridazine ring revealed numerous permissive substitutions, and detailed SAR studies were carried out in this portion of the molecule. Replacement of the ...