81016-46-8Relevant academic research and scientific papers
1H-pyrazolo[2,3-d][1,2,4]triazine-3,7-diones as a new class of Human Leukocyte Elastase inhibitors
Baraldi, Pier Giovanni,Cacciari, Barbara,Romagnoli, Romeo,Spalluto, Giampiero
, p. 997 - 1000 (2007/10/03)
A novel series of 1H-2-phenyl-substituted-pyrazolo[2,3- d][l,2,4]triazine-3,7-diones (3a-g) as potential inhibitors of Human Leukocyte Elastase (HLE) are reported, the acyl-pyrazole being probably involved in the inhibition mechanism of the serino-protease enzymes. The most potent inhibitor both in vivo and in vitro was 2-o-methoxyphenyl-5-methyl-6- nitro-pyrazolo[2,3-d][1,2,4]triazine-3,7-dione (3e), which significantly suppressed the HLE-induced pulmonary injury in rats when administered orally (100 mg/kg, 3 h prior to HLE administration.
