Document Detail


NO donors with antithrombotic and vasodilating activities, Part 23. Organic azides.
MedLine Citation:
PMID:  9713253     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Twenty eight organic azides were synthesized and tested for their antithrombotic and blood pressure lowering activities in rats (60 mg/kg, p.o.). In fifteen compounds significant antithrombotic effects were observed. In thirteen cases a significant lowering of the blood pressure of spontaneously hypertensive rats (SHR) was seen. The peak activities in both systems were found for hexyl azide (4), 2-phenylethyl azide (14), and 4-pyridinecarboxylic acid azide (23). In these compounds the inhibition of thrombus formation in mesenteric arterioles was > 20%. The lowering of blood pressure was > 10% and long lasting (> 6 h) in 4 and 14 while 23 had a shorter duration of action (approximately 4 h). In two classes of azides, namely branched aliphatic azides (e.g. 2-azidopentane 9) and aliphatic carbonyl derivatives (e.g. benzoyl-azido-methane 17), only antithrombotic properties were observed. A lack of endothelial metabolism is suggested to be the reason for this therapeutically favorable behaviour.
Authors:
K Satyanarayana; K Rehse
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Archiv der Pharmazie     Volume:  331     ISSN:  0365-6233     ISO Abbreviation:  Arch. Pharm. (Weinheim)     Publication Date:  1998 Jun 
Date Detail:
Created Date:  1998-09-16     Completed Date:  1998-09-16     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0330167     Medline TA:  Arch Pharm (Weinheim)     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  207-10     Citation Subset:  IM    
Affiliation:
Institut für Pharmazie I, Freie Universität Berlin, Germany.
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MeSH Terms
Descriptor/Qualifier:
Animals
Azides / chemical synthesis*,  therapeutic use
Blood Pressure / drug effects*
Fibrinolytic Agents / chemical synthesis*,  therapeutic use
Humans
Hypertension / drug therapy
Nitric Oxide / metabolism*,  pharmacology
Platelet Aggregation Inhibitors / chemical synthesis*,  pharmacology
Rats
Rats, Inbred SHR
Structure-Activity Relationship
Vasodilator Agents / chemical synthesis*,  therapeutic use
Chemical
Reg. No./Substance:
0/Azides; 0/Fibrinolytic Agents; 0/Platelet Aggregation Inhibitors; 0/Vasodilator Agents; 10102-43-9/Nitric Oxide

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