Document Detail


Synthesis and evaluation of anthranilic acid-based transthyretin amyloid fibril inhibitors.
MedLine Citation:
PMID:  9990446     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Eight small molecules were synthesized to evaluate the structure activity relationships (SAR) of N-substituted anthranilic acids. The molecules were synthesized by benzylation or arylation of methyl anthranilate. A light scattering-based amyloid fibril formation assay was used to evaluate potential inhibitors of transthyretin (TTR) amyloid fibril formation in vitro. The m-carboxyphenylated and o-trifluoromethylphenylated anthranilic acids are potent inhibitors that will be subjected to further SAR and structural analysis.
Authors:
V B Oza; H M Petrassi; H E Purkey; J W Kelly
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  9     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  1999 Jan 
Date Detail:
Created Date:  1999-04-13     Completed Date:  1999-04-13     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  1-6     Citation Subset:  IM    
Affiliation:
Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, USA.
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MeSH Terms
Descriptor/Qualifier:
Amyloid / antagonists & inhibitors*
Anthranilic Acids / chemistry*,  metabolism,  pharmacology*
Binding Sites
Drug Evaluation, Preclinical
Flufenamic Acid / chemistry*,  metabolism,  pharmacology*
Humans
Light
Molecular Structure
Prealbumin / drug effects*,  metabolism*
Protein Conformation
Protein Folding
Scattering, Radiation
Structure-Activity Relationship
Grant Support
ID/Acronym/Agency:
R01 DK46335/DK/NIDDK NIH HHS
Chemical
Reg. No./Substance:
0/Amyloid; 0/Anthranilic Acids; 0/Prealbumin; 27693-67-0/N-(3-carboxyphenyl)anthranilic acid; 530-78-9/Flufenamic Acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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