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  • Zhang, Mei, et al. (author)
  • Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement
  • 2012
  • In: ACS Medicinal Chemistry Letters. - : American Chemical Society (ACS). - 1948-5875. ; 3:4, s. 317-321
  • Journal article (peer-reviewed)abstract
    • 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, 7I, and 7o) greatly improving their activity. Optimized compound 7I has an excellent inhibition activity with IC50 values as low as 13 nM. We demonstrated that the compound 7I inhibited C9 deposition through the classical, the lectin, and the alternative pathways but had no influence on C3 and C4 depositions.
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Type of publication
journal article (1)
Type of content
peer-reviewed (1)
Author/Editor
Blom, Anna (1)
Li, Jia (1)
Groeneveld, Tom (1)
Zhang, Mei (1)
Lu, Wei (1)
Tang, Wei (1)
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Yang, Xiao-Ying (1)
He, Pei-Lan (1)
Zhu, Feng-Hua (1)
Zuo, Jian-Ping (1)
Nan, Fa-Jun (1)
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University
Lund University (1)
Language
English (1)
Research subject (UKÄ/SCB)
Medical and Health Sciences (1)
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