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.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 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.