Abstract
The synthesis, analgesic and anti-inflammatory activity of 3-aryl(heteryl)-2-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)-acrylonitrile derivatives.
Highlights
A series of new 3-(het)aryl-2-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)acrylonitrile derivatives can be synthesized by the interaction of 2-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin3-yl)acetonitrile witharenecarbaldehydes
Because of the weak effect on thromboxane and kidney prostaglandins this group of drugs is characterized by drawbacks for the cardiovascular system and other undesirable reactions [1, 3, 4]. These facts reveal the importance of searching for new non-steroid anti-inflammatory drugs (NSAIDs), which are safer and more effective than the existing analogs
A series of new 3-(het)aryl-2-(6,7,8,9-tetrahydro5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)acrylonitrile derivatives can be synthesized by the interaction of 2-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)acetonitrile witharenecarbaldehydes
Summary
Condensation of 2-methoxy-3,4,5,6-tetrahydro-7H-azepine with cyanoacetic acid hydrazide leads to formation of 2-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)acetonitrile. One of the compounds synthesized, namely 3-(4-hydroxyphenyl)-2-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)acrylonitrile, exhibits a high level of the analgesic activity on the “hot plate” model, and a similar level of the activity on the model of “acetic acid-induced writhings” as compared to ketorolac. The analgesic and anti-inflammatory activities of 3-(4-hydroxyphenyl)-2-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)acrylonitrile were determined using models of “carrageenan induced paw edema”, ”hot plate” and “acetic acid-induced writhings”, and compared to the reference drug ketorolac
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