1362623-29-7Relevant academic research and scientific papers
COMPLEMENT MODULATORS AND RELATED METHODS
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Paragraph 0415-0416, (2020/10/20)
The present disclosure presents compounds and compositions that interact with complement components. Some compounds inhibit complement activity. Included are small molecule compounds and compositions that function as C5 inhibitor compounds. Methods for inhibiting complement activity and methods of treating complement-related indications with the C5 inhibitor compounds and compositions are provided.
Discovery and structural modification of 1-phenyl-3-(1-phenylethyl)urea derivatives as inhibitors of complement
Zhang, Mei,Yang, Xiao-Ying,Tang, Wei,Groeneveld, Tom W. L.,He, Pei-Lan,Zhu, Feng-Hua,Li, Jia,Lu, Wei,Blom, Anna M.,Zuo, Jian-Ping,Nan, Fa-Jun
, p. 317 - 321 (2012/05/20)
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.
