Document Detail


Design and synthesis of 1-(4-benzoylphenyl)imidazole derivatives as new potent 20-HETE synthase inhibitors.
MedLine Citation:
PMID:  15454216     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Structural modification of the novel 20-HETE synthase inhibitor 1 (IC(50) 310nM) is described. Introduction of a side chain with a carboxylic acid at the terminal position to 1 resulted in increased ability to inhibit human renal microsomal production of 20-HETE (7c: IC(50) 7.9nM), with good selectivity toward CYP2D6 and cyclooxygenases (COX)-1 and -2.
Authors:
Toshio Nakamura; Takaaki Ishii; Noriyuki Miyata; Kazuo Taniguchi; Yasumitsu Tomishima; Tomokazu Ueki; Masakazu Sato
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  14     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2004 Nov 
Date Detail:
Created Date:  2004-09-29     Completed Date:  2005-05-05     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:  5305-8     Citation Subset:  IM    
Affiliation:
Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd, 403, Yoshino-Cho 1-Chome, Kita-ku, Saitama-Shi, Saitama 331-9530, Japan. toshio.nakamura@po.rd.taisho.co.jp
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MeSH Terms
Descriptor/Qualifier:
Animals
Cytochrome P-450 Enzyme System / antagonists & inhibitors*
Humans
Hydroxyeicosatetraenoic Acids / antagonists & inhibitors*,  metabolism
Imidazoles / chemical synthesis*,  chemistry,  pharmacology
Kidney / metabolism,  ultrastructure
Microsomes / metabolism
Models, Molecular
Molecular Structure
Rats
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Hydroxyeicosatetraenoic Acids; 0/Imidazoles; 79551-86-3/20-hydroxy-5,8,11,14-eicosatetraenoic acid; 9035-51-2/Cytochrome P-450 Enzyme System

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