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Tetrahedron letters

MAOS protocols for the general synthesis and lead optimization of 3, 6-disubstituted-[1, 2, 4] triazolo [4, 3-b] pyridazines

…, EP Lebois, LM Lewis, NT Nalywajko, CM Niswender…

文献索引:Aldrich, Leslie N.; Lebois, Evan P.; Michelle Lewis; Nalywajko, Natalia T.; Niswender, Colleen M.; David Weaver; Jeffrey Conn; Lindsley, Craig W. Tetrahedron Letters, 2009 , vol. 50, # 2 p. 212 - 215

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被引用次数: 14

摘要

General, high-yielding MAOS protocols for the expedient synthesis of functionalized 3, 6- disubstituted-[1, 2, 4] triazolo [4, 3-b] pyridazines are described amenable to an iterative analog library synthesis strategy for the lead optimization of an M1 antagonist screening hit. Optimized compounds proved to be highly selective M1 antagonists.