32683-00-4Relevant articles and documents
COMPOUNDS AND USES THEREOF
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, (2018/05/17)
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
Imidazole-derived agonists for the neurotensin 1 receptor
Hershberger, Paul M.,Hedrick, Michael P.,Peddibhotla, Satyamaheshwar,Mangravita-Novo, Arianna,Gosalia, Palak,Li, Yujie,Gray, Wilson,Vicchiarelli, Michael,Smith, Layton H.,Chung, Thomas D.Y.,Thomas, James B.,Caron, Marc G.,Pinkerton, Anthony B.,Barak, Lawrence S.,Roth, Gregory P.
supporting information, p. 262 - 267 (2014/01/17)
A scaffold-hop program seeking full agonists of the neurotensin-1 (NTR1) receptor identified the probe molecule ML301 (1) and associated analogs, including its naphthyl analog (14) which exhibited similar properties. Compound 1 showed full agonist behavior (79-93%) with an EC50 of 2.0-4.1 μM against NTR1. Compound 1 also showed good activity in a Ca mobilization FLIPR assay (93% efficacy at 298 nM), consistent with it functioning via the G q coupled pathway, and good selectivity relative to NTR2 and GPR35. In further profiling, 1 showed low potential for promiscuity and good overall pharmacological data. This report describes the discovery, synthesis, and SAR of 1 and associated analogs. Initial in vitro pharmacologic characterization is also presented.
Highly efficient oxidation of 2-imidazoline-5-carboxylic derivatives to imidazole-5-carboxylic derivatives by dioxygen
Huang, Yue,Zu, Xiaodong,Wu, Fan,Xu, Jinyi,Wu, Xiaoming,Yao, Hequan
supporting information; experimental part, p. 3123 - 3128 (2012/06/01)
A highly efficient and environmental-benign oxidation by dioxygen (or air) as the sole oxidant was first applied for the conversion of 2-imidazoline-5- carboxylic derivatives to imidazole-5-carboxylic derivatives in very good and excellent yields. The sub