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Discovery and Struc...
Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement
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Zhang, Mei (author)
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Yang, Xiao-Ying (author)
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Tang, Wei (author)
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- Groeneveld, Tom (author)
- Lund University,Lunds universitet,Proteinkemi, Malmö,Forskargrupper vid Lunds universitet,Protein Chemistry, Malmö,Lund University Research Groups
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He, Pei-Lan (author)
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Zhu, Feng-Hua (author)
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Li, Jia (author)
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Lu, Wei (author)
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- Blom, Anna (author)
- Lund University,Lunds universitet,Proteinkemi, Malmö,Forskargrupper vid Lunds universitet,Protein Chemistry, Malmö,Lund University Research Groups
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Zuo, Jian-Ping (author)
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Nan, Fa-Jun (author)
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(creator_code:org_t)
- 2012-02-29
- 2012
- English.
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In: ACS Medicinal Chemistry Letters. - : American Chemical Society (ACS). - 1948-5875. ; 3:4, s. 317-321
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http://dx.doi.org/10...
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https://europepmc.or...
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Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Keyword
- high-throughput screening
- structural modification
- complement
- inhibitors
- C9
Publication and Content Type
- art (subject category)
- ref (subject category)
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To the university's database
- By the author/editor
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Zhang, Mei
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Yang, Xiao-Ying
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Tang, Wei
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Groeneveld, Tom
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He, Pei-Lan
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Zhu, Feng-Hua
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show more...
-
Li, Jia
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Lu, Wei
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Blom, Anna
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Zuo, Jian-Ping
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Nan, Fa-Jun
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
- Articles in the publication
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ACS Medicinal Ch ...
- By the university
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Lund University