Mojzych Mariusz, Kubacka Monika, Mogilski Szczepan, Filipek Barbara, Fornal Emilia
a Department of Chemistry , Siedlce University of Natural Sciences and Humanities , Siedlce , Poland .
b Department of Pharmacodynamics , Jagiellonian University Medical College , Kraków , Poland , and.
J Enzyme Inhib Med Chem. 2016;31(3):381-8. doi: 10.3109/14756366.2015.1024674. Epub 2015 Mar 23.
A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine with chiral amino group has been synthesized and characterized. The compounds were tested for their relaxant effects in the rat aorta. Evaluation of prepared derivatives demonstrated that compound (8a) is probably a non-selective phosphodiesterase (PDE) inhibitor, as it induced aortic relaxation through endothelium-independent mechanism.
合成并表征了一系列新型含手性氨基的吡唑并[4,3-e][1,2,4]三嗪磺酰胺衍生物。测试了这些化合物对大鼠主动脉的舒张作用。对所制备衍生物的评估表明，化合物(8a)可能是一种非选择性磷酸二酯酶(PDE)抑制剂，因为它通过不依赖内皮的机制诱导主动脉舒张。
