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


AUTHORS

Aldrich LNLeslie N , Lebois EP Evan P , Lewis LM L Michelle , Nalywajko NT Natalia T , Niswender CM Colleen M , Weaver CD C David , Conn PJ P Jeffrey , Lindsley CW Craig W . Tetrahedron letters. 2009 1 14; 50(2). 212-215

ABSTRACT

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.


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.