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10.1021/ml300005w

http://scihub22266oqcxt.onion/10.1021/ml300005w
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suck abstract from ncbi


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pmid24900471
      ACS+Med+Chem+Lett 2012 ; 3 (4 ): 317-21
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  • Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement #MMPMID24900471
  • Zhang M ; Yang XY ; Tang W ; Groeneveld TW ; He PL ; Zhu FH ; Li J ; Lu W ; Blom AM ; Zuo JP ; Nan FJ
  • ACS Med Chem Lett 2012[Apr]; 3 (4 ): 317-21 PMID24900471 show ga
  • 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 activity with IC50 values as low as 13 nM. We demonstrated that the compound 7l 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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