| Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists. | |
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MedLine Citation:
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PMID: 18595693 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A series of aniline-substituted tetrahydroquinoline C5a receptor antagonists were discovered. A functionality requirement of ortho substitution on the aniline was revealed. Secondary anilines, in general, outperformed tertiary analogs in inhibition of C5a-induced calcium mobilization. Further enhancement of activity was realized in the presence of an ortho hydroxyalkyl side chain. The functional IC(50) of selected analogs was optimized to the single-digit nanomolar level. |
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Authors:
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Yong Gong; J Kent Barbay; Mieke Buntinx; Jian Li; Jean Van Wauwe; Concha Claes; Guy Van Lommen; Pamela J Hornby; Wei He |
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Publication Detail:
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Type: Journal Article Date: 2008-06-20 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 18 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2008 Jul |
Date Detail:
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Created Date: 2008-07-21 Completed Date: 2008-11-17 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 3852-5 Citation Subset: IM |
Affiliation:
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Johnson & Johnson Pharmaceutical Research and Development, Spring House, PA 19477-0776, USA. ygong@prdus.jnj.com |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Aniline Compounds
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chemistry* Binding Sites Chemistry, Pharmaceutical / methods Drug Design Humans Inhibitory Concentration 50 Ligands Models, Chemical Molecular Conformation Molecular Structure Quinolines / chemistry* Receptor, Anaphylatoxin C5a / antagonists & inhibitors* Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Aniline Compounds; 0/Ligands; 0/Quinolines; 0/Receptor, Anaphylatoxin C5a; 62-53-3/aniline |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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