845552-76-3Relevant articles and documents
Process Development for the Synthesis of a Selective M1 and M4 Muscarinic Acetylcholine Receptors Agonist
Uruno, Yoshiharu,Hashimoto, Kazuki,Hiyama, Yoichi,Sumiyoshi, Takaaki
, p. 1610 - 1615 (2017)
A practical and chromatography-free synthetic process to selective M1 and M4 muscarinic acetylcholine receptors agonist was developed and demonstrated on a several hundred gram scale. The key feature of this route is N,N-dimethylcarb
Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists
Takai, Kentaro,Inoue, Yasunao,Konishi, Yasuko,Suwa, Atsushi,Uruno, Yoshiharu,Matsuda, Harumi,Nakako, Tomokazu,Sakai, Mutsuko,Nishikawa, Hiroyuki,Hashimoto, Gakuji,Enomoto, Takeshi,Kitamura, Atsushi,Uematsu, Yasuaki,Kiyoshi, Akihiko,Sumiyoshi, Takaaki
, p. 3189 - 3193 (2014/06/24)
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.