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ID: ALA3351422
Journal: Bioorg Med Chem Lett
Title: Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists.
Authors: Takai K, Inoue Y, Konishi Y, Suwa A, Uruno Y, Matsuda H, Nakako T, Sakai M, Nishikawa H, Hashimoto G, Enomoto T, Kitamura A, Uematsu Y, Kiyoshi A, Sumiyoshi T.
Abstract: We designed and synthesized novel N-substituted 7-azaindoline derivatives as selective M1 and M4 muscarinic acetylcholine receptors (mAChRs) agonists. Hybridization of compound 2 with the HTS hit compound 5 followed by optimization of the N-substituents of 7-azaindoline led to identification of compound 1, which showed highly selective M1 and M4 mAChRs agonistic activity, weak human ether-a-go-go related gene inhibition, and good bioavailability in multiple animal species.
CiteXplore: 24856064