Document Detail

Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
MedLine Citation:
PMID:  7310827     Owner:  NLM     Status:  MEDLINE    
In our continuing effort to discover compound which inhibit collagen-induced platelet aggregation, we have screened compounds in a mouse pulmonary thromboembolism screen. Methyl 4,5-bis(4-methoxyphenyl)-2-thiazoleacetate (3) was very active in the above screen. However, 3 was active for less than 5 min when given orally to guinea pigs. As a result, our synthetic goal was to prepare 2-substituted thiazoles with a much longer duration of activity. This paper describes the preparation of a number 4,5-bis(aryl)-2-substituted-thiazoles and their in vitro and ex vivo activity against collagen-induced platelet aggregation. It was determined that 4,5-bis(4-methoxyphenyl)-2-(trifluoromethyl)thiazole (16) is the most promising compound.
R H Rynbrandt; E E Nishizawa; D P Balogoyen; A R Mendoza; K A Annis
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  24     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  1981 Dec 
Date Detail:
Created Date:  1982-02-22     Completed Date:  1982-02-22     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1507-10     Citation Subset:  IM    
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MeSH Terms
Chemical Phenomena
Guinea Pigs
Platelet Aggregation / drug effects*
Thiazoles / chemical synthesis*,  pharmacology
Thromboembolism / prevention & control
Reg. No./Substance:

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