- 1H-pyrazolo[2,3-d][1,2,4]triazine-3,7-diones as a new class of Human Leukocyte Elastase inhibitors
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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.
- Baraldi, Pier Giovanni,Cacciari, Barbara,Romagnoli, Romeo,Spalluto, Giampiero
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p. 997 - 1000
(2007/10/03)
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