Document Detail

Imidazo[1,2-alpha]pyridines. III. Synthesis and bradycardic activity of new 5-imidazo[1,2-alpha]pyridin-6-ylpyridine derivatives.
MedLine Citation:
PMID:  1394667     Owner:  NLM     Status:  MEDLINE    
Structural modification of the cardiotonic agent, loprinone (E-1020, 1), suggested by data that it has a less positive chronotropic effect than milrinone (15), led us to find novel bradycardic agents that were structurally different from homoveratryl amine derivatives. Alkyl-oxy, -thio, and -amino derivatives at the 2-position of the pyridine ring of 1 produced bradycardic activity without a significant effect on blood pressure and myocardial contractility. Aryloxy analogues also decreased heart rate, and members with an electron-withdrawing group at the ortho position of the phenyl ring showed higher activity. Replacement of the imidazo[1,2-alpha]pyridine with pyridine resulted in diminished activity. The mechanism of bradycardic activity of these compounds seems to be direct action on the sinus node.
M Yamanaka; S Suda; Y Kabasawa; T Kawamura; T Ogawa; K Sawada; H Ohhara
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Chemical & pharmaceutical bulletin     Volume:  40     ISSN:  0009-2363     ISO Abbreviation:  Chem. Pharm. Bull.     Publication Date:  1992 Jun 
Date Detail:
Created Date:  1992-11-04     Completed Date:  1992-11-04     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0377775     Medline TA:  Chem Pharm Bull (Tokyo)     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  1486-93     Citation Subset:  IM    
Eisai Tsukuba Research Laboratories, Ibaraki, Japan.
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MeSH Terms
Guinea Pigs
Heart Rate / drug effects*
Imidazoles / chemical synthesis,  pharmacology*
Pyridines / chemical synthesis,  pharmacology*
Structure-Activity Relationship
Reg. No./Substance:
0/Imidazoles; 0/Pyridines

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