Discovery and structural modification of 1-phenyl-3-(1-phenylethyl) urea derivatives as inhibitors of complement

…, XY Yang, W Tang, TWL Groeneveld…

文献索引：Zhang, Mei; Yang, Xiao-Ying; Tang, Wei; Groeneveld, Tom W. L.; He, Pei-Lan; Zhu, Feng-Hua; Li, Jia; Lu, Wei; Blom, Anna M.; Zuo, Jian-Ping; Nan, Fa-Jun ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 4 p. 317 - 321

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被引用次数: 2

摘要

A series of 1-phenyl-3-(1-phenylethyl) urea derivatives were identified as novel and potent complement inhibitors through structural modification of the original compound from high- throughput screening. Various analogues (7 and 13–15) were synthesized and identified as complement inhibitors, with the introduction of a five-or six-carbon chain (7c, 7d, 7k, 7l, and 7o) greatly improving their activity. Optimized compound 7l has an excellent inhibition ...