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
- PMID: 22090663[PubMed].
- PMCID: PMC3214729.
- NIHMSID: NIHMS94278
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.