Document Detail

Synthesis of indolylalkoxyiminoalkylcarboxylates as leukotriene biosynthesis inhibitors.
MedLine Citation:
PMID:  9113329     Owner:  NLM     Status:  MEDLINE    
A series of substituted indolylalkoxyiminoalkylcarboxylates were found to be potent leukotriene biosynthesis inhibitors. The structure-activity relationships were investigated. Representative potent inhibitors identified were the quinolyl 3a (A-86885) and pyridyl 3b (A-86886) congeners with in vitro IC50s of 21 and 9 nM and in vivo leukotriene inhibition in the rat with oral ED50s of 0.9 and 1.7 mg/kg, respectively.
T Kolasa; P Bhatia; C D Brooks; K I Hulkower; J B Bouska; R R Harris; R L Bell
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  5     ISSN:  0968-0896     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  1997 Mar 
Date Detail:
Created Date:  1997-08-18     Completed Date:  1997-08-18     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  507-14     Citation Subset:  IM    
Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
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MeSH Terms
Carrier Proteins / metabolism
Indoles / chemical synthesis,  chemistry*,  pharmacology
Leukotriene Antagonists
Leukotrienes / biosynthesis*
Lipoxygenase Inhibitors / chemical synthesis,  chemistry*,  pharmacology
Magnetic Resonance Spectroscopy
Membrane Proteins / metabolism
Models, Chemical
Quinolines / chemical synthesis,  chemistry*,  pharmacology
Structure-Activity Relationship
Reg. No./Substance:
0/5-lipoxygenase-activating protein; 0/Carrier Proteins; 0/Indoles; 0/Leukotriene Antagonists; 0/Leukotrienes; 0/Lipoxygenase Inhibitors; 0/Membrane Proteins; 0/Quinolines; 136668-42-3/MK 0591

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