Synthesis and preliminary pharmacological investigation of some 2-[4-(dialkylaminoalkoxy)phenyl]benzotriazoles and their N-oxides.
A set of 2-[4-(dialkylaminoalkoxy)phenyl]benzotriazoles and corresponding N-oxides was prepared. In a preliminary pharmacological investigation concerning some of these compounds, several in vitro and in vivo activities were shown. At concentrations in the range of 3-10 microM all tested compounds strongly inhibited (50-100%) the guinea pig ileum contractions induced either electrically or by means of several agonists; of particular interest was the antagonism to leukotriene D4. Compound 5b inhibited platelet aggregation induced by thromboxane A2, PAF and ADF (but not by arachidonic acid) and increased the bleeding time in mice. Compounds 5b and 6b protected mice from potassium cyanide hypoxia and exerted anti-hypercholesterolemic action; the first compound produced a ratio between HPL and total serum cholesterol concentrations below 0.92, thus indicating a potential anti-atherogenic activity.
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Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Italy.
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D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D066298:In Vitro Techniques; D017998:Leukotriene D4 / Q000037:antagonists & inhibitors*; D008297:Male; D051379:Mice; D051381:Rats; D013928:Thromboxane A2 / Q000037:antagonists & inhibitors*; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000924:Anticholesteremic Agents; D014230:Triazoles; D013928:Thromboxane A2; D017998:Leukotriene D4; C012771:benzotriazole