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

Leslie N Aldrich; Evan P Lebois; L Michelle Lewis; Natalia T Nalywajko; Colleen M Niswender; C David Weaver; P Jeffrey Conn; Craig W Lindsley

doi:10.1016/j.tetlet.2008.10.127

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

Tetrahedron Lett. 2009 Jan 14;50(2):212-215. doi: 10.1016/j.tetlet.2008.10.127.

Authors

Leslie N Aldrich¹, Evan P Lebois, L Michelle Lewis, Natalia T Nalywajko, Colleen M Niswender, C David Weaver, P Jeffrey Conn, Craig W Lindsley

Affiliation

¹ Department of Chemistry, Vanderbilt University and Medical Center, Nashville, TN 37232, USA.

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.

Abstract

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