Synthesis and antipancreatitis activities of novel N-(2-sulfonylamino-5-trifluoromethyl-3-pyridyl)carboxamide derivatives as phospholipase A2 inhibitors.
Novel N-(2-sulfonylamino-5-trifluoromethyl-3-pyridyl)carboxamide derivatives have been prepared and evaluated as phospholipase A2 (PLA2) inhibitors. Among these compounds, IS-741 (sodium salt of 1j), which showed the highest and the most stable therapeutic effect on acute hemorrhagic pancreatitis induced by the closed duodenal loop method in rats, was selected as a candidate for further development.
Kimura
H
H
Central Research Institute, Ishihara Sangyo Kaisha, Ltd., Shiga, Japan.
Yotsuya
S
S
Yuki
S
S
Sugi
H
H
Shigehara
I
I
Haga
T
T
D000208:Acute Disease; D000577:Amides / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D010195:Pancreatitis / Q000188:drug therapy*; D010741:Phospholipases A / Q000037:antagonists & inhibitors*; D054467:Phospholipases A2; D011725:Pyridines / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley
D000577:Amides; D004791:Enzyme Inhibitors; D011725:Pyridines; C097462:IS 741; D010741:Phospholipases A; D054467:Phospholipases A2