Document Detail

Structure-activity relationships of novel anti-malarial agents: part 5. N-(4-acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.
MedLine Citation:
PMID:  12565929     Owner:  NLM     Status:  MEDLINE    
We have developed the [5-(4-nitrophenyl)-2-furyl]acrylic acid substituted benzophenone 4g as a novel lead for anti-malarial agents. Here, we demonstrated that the acyl residue at the 2-amino group of the benzophenone core structure has to be a phenylacetic acid substructure substituted in its para-position with methyl or other substituents of similar size. The trifluoromethyl substituted derivative displayed an IC(50) of 47 nM against the multi-drug resistant Plasmodium falciparum strain Dd2.
Jochen Wiesner; Katja Kettler; Jacek Sakowski; Regina Ortmann; Hassan Jomaa; Martin Schlitzer
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  13     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2003 Feb 
Date Detail:
Created Date:  2003-02-04     Completed Date:  2003-08-15     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  361-3     Citation Subset:  IM    
Biochemisches Institut der Universitätsklinik Giessen, Friedrichstrasse 24, Giessen, Germany.
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MeSH Terms
Acrylates / chemical synthesis*,  pharmacology
Antimalarials / chemical synthesis*,  pharmacology
Drug Resistance, Multiple
Erythrocytes / drug effects,  parasitology
Furans / chemical synthesis*,  pharmacology
Indicators and Reagents
Plasmodium falciparum / drug effects
Structure-Activity Relationship
Reg. No./Substance:
0/Acrylates; 0/Antimalarials; 0/Furans; 0/Indicators and Reagents; 0/N-(4-acylamino-3-benzoylphenyl)-(5-(4-nitrophenyl)-2-furyl)acrylic acid amide

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