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Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement

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Author

  • Mei Zhang
  • Xiao-Ying Yang
  • Wei Tang
  • Tom Groeneveld
  • Pei-Lan He
  • Feng-Hua Zhu
  • Jia Li
  • Wei Lu
  • Anna Blom
  • Jian-Ping Zuo
  • Fa-Jun Nan
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Summary, in English

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.

Publishing year

2012

Language

English

Pages

317-321

Publication/Series

ACS Medicinal Chemistry Letters

Volume

3

Issue

4

Document type

Journal article

Publisher

The American Chemical Society (ACS)

Topic

  • Medicinal Chemistry

Keywords

  • high-throughput screening
  • structural modification
  • complement
  • inhibitors
  • C9

Status

Published

Research group

  • Protein Chemistry, Malmö

ISBN/ISSN/Other

  • ISSN: 1948-5875