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New NO‐Donors with Antithrombotic and Vasodilating Activities, Part 14 1,3,4‐Triazol‐1‐oles
Author(s) -
Rehse Klaus,
Piechocki Daniela,
Schober Markus,
Scheffler Heike,
Reitner Nora,
Unsöld E.
Publication year - 1996
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19963291107
Subject(s) - antithrombotic , chemistry , nitric oxide , thrombus , pharmacology , mechanism of action , vasodilation , oxime , stereochemistry , aryl , alkyl , medicinal chemistry , in vitro , biochemistry , organic chemistry , medicine
Five 1,3,4‐triazol‐1‐oles ( 5a—f ) with different alkyl, aryl, and arylalkyl substituents in 2,5‐position were synthesized and tested for their antithrombotic properties. The 2,5‐dimethyl derivative 5a was most active. 2 h after administration of 60 mg/kg to rats thrombus formation by a laser beam was inhibited by 42 % in arterioles and by 33 % in venules. At the same dose the blood pressure of SHR rats was slightly (5%) but significantly decreased even 4 h after application of 5a . This pattern of activities suggests a nitric oxide mediated mechanism of action. 1,1′‐Azo‐bis‐ethanone oxime ( 7 ) — the synthetic precursor of 5a — inhibited the aggregation of blood platelet (Born test) with an IC 50 = 15 μmol/L.