Document Detail


Preparation of 2- and 4-(2-alkylcarbamoyl-1-methylvinyl)-7-alkyloxybenzo[b]furans having potent antagonistic activity against human leukotriene B4 BLT1 and/or BLT2 receptors.
MedLine Citation:
PMID:  15565232     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
(E)-2-Acetyl-4-(2-diethylcarbamoyl-1-methylvinyl)-7-(1-phenylethoxy)benzo[b]furan (4b) with a characteristic conformation and (E)-2-(2-morpholinocarbo-1-methylvinyl)-7-ethoxycarbopropoxybenzo[b]furan ((E)-3b) were prepared and evaluated for their leukotriene B4(LTB4) antagonistic activity. Compound 4b showed potent antagonistic activity against human BLT1 and BLT2 receptors. Compound (E)-3b displayed selective BLT2 receptor antagonistic activity. Both compounds were inactive to cysteinyl LT receptors.
Authors:
Kumiko Ando; Eriko Tsuji; Yuko Ando; Jun-ichi Kunitomo; Masayuki Yamashita; Shunsaku Ohta; Takeshi Nabe; Shigekatsu Kohno; Takehiko Yokomizo; Takao Shimizu; Yoshitaka Ohishi
Publication Detail:
Type:  Journal Article     Date:  2004-11-01
Journal Detail:
Title:  Organic & biomolecular chemistry     Volume:  2     ISSN:  1477-0520     ISO Abbreviation:  Org. Biomol. Chem.     Publication Date:  2004 Dec 
Date Detail:
Created Date:  2004-11-26     Completed Date:  2005-02-03     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  101154995     Medline TA:  Org Biomol Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  3427-31     Citation Subset:  IM    
Affiliation:
School of Pharmaceutical Sciences, Mukogawa Women's University, 11-68 Koshien Kyuban-cho, Nishinomiya, 663-8179, Japan.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Animals
Benzofurans / chemical synthesis*,  chemistry,  pharmacology*
CHO Cells
Calcium / metabolism
Calcium Signaling / drug effects
Carbamates / chemical synthesis*,  chemistry,  pharmacology*
Cricetinae
Crystallography, X-Ray
Gene Expression
Humans
Inhibitory Concentration 50
Molecular Conformation
Molecular Structure
Morpholines / chemical synthesis*,  chemistry,  pharmacology*
Receptors, Leukotriene B4 / antagonists & inhibitors*,  genetics,  metabolism
Receptors, Purinergic P2 / antagonists & inhibitors*,  genetics,  metabolism
Chemical
Reg. No./Substance:
0/2-(2-morpholinocarbo-1-methylvinyl)-7-ethoxycarbopropoxybenzo(b)furan; 0/2-acetyl-4-(2-diethylcarbamoyl-1-methylvinyl)-7-(1-phenylethoxy)benzo(b)furan; 0/Benzofurans; 0/Carbamates; 0/LTB4R protein, human; 0/LTB4R2 protein, human; 0/Morpholines; 0/Receptors, Leukotriene B4; 0/Receptors, Purinergic P2; 7440-70-2/Calcium

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


Previous Document:  Multivalency in supramolecular chemistry and nanofabrication.
Next Document:  Self-replication vs. reactive binary complexes--manipulating recognition-mediated cycloadditions by ...