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

In English

Författare

  • 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
Visa allt

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.

Publiceringsår

2012

Språk

Engelska

Sidor

317-321

Publikation/Tidskrift/Serie

ACS Medicinal Chemistry Letters

Volym

3

Issue

4

Dokumenttyp

Artikel i tidskrift

Förlag

The American Chemical Society (ACS)

Ämne

  • Medicinal Chemistry

Nyckelord

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

Status

Published

Forskningsgrupp

  • Protein Chemistry, Malmö

ISBN/ISSN/Övrigt

  • ISSN: 1948-5875