Aryl 1, 4-diazepane compounds as potent and selective CB2 agonists: Optimization of drug-like properties and target independent parameters

…, CL Fullenwider, H Grbic, P Kaplita, B Linehan…

文献索引：Zindell, Renee; Walker, Edward R.; Scott, John; Amouzegh, Patricia; Wu, Lifen; Ermann, Monika; Thomson, David; Fisher, Micheal B.; Fullenwider, Cody Lee; Grbic, Heather; Kaplita, Paul; Linehan, Brian; Patel, Mita; Patel, Monica; Loebbe, Sabine; Block, Svenja; Albrecht, Claudia; Gemkow, Mark J.; Shih, Daw-Tsun; Riether, Doris Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 14 p. 4276 - 4280

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被引用次数: 9

摘要

Abstract A high throughput screening campaign identified aryl 1, 4-diazepane compounds as potent and selective cannabinoid receptor 2 agonists as compared to cannabinoid receptor 1. This class of compounds suffered from poor drug-like parameters as well as low microsomal stability and poor solubility. Structure–activity relationships are described with a focus on improving the drug-like parameters resulting in compounds with improved ...