Structure–activity relationships for 1-alkyl-3-(1-naphthoyl) indoles at the cannabinoid CB 1 and CB 2 receptors: steric and electronic effects of naphthoyl substituents. …

…, K Bushell, ALS Thompson, S Bushell, C Tartal…

文献索引：Huffman, John W.; Zengin, Gulay; Wu, Ming-Jung; Lu, Jianzhong; Hynd, George; Bushell, Kristen; Thompson, Alicia L.S.; Bushell, Simon; Tartal, Cindy; Hurst, Dow P.; Reggio, Patricia H.; Selley, Dana E.; Cassidy, Michael P.; Wiley, Jenny L.; Martin, Billy R. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 1 p. 89 - 112

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被引用次数: 203

摘要

In an effort to improve indole-based CB2 cannabinoid receptor ligands and also to develop SAR for both the CB1 and CB2 receptors, 47 indole derivatives were prepared and their CB1 and CB2 receptor affinities were determined. The indole derivatives include 1-propyl- and 1-pentyl-3-(1-naphthoyl) indoles both with and without a 2-methyl substituent. Naphthoyl substituents include 4-and 7-alkyl groups as well as 2-, 4-, 6-, 7-methoxy and 4- ...