55159-77-8Relevant articles and documents
Evaluation of pyrrolin-2-one derivatives synthesized by a new practical method as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Miyazaki, Hiroshi,Miyake, Tsutomu,Terakawa, Yoshihiro,Ohmizu, Hiroshi,Ogiku, Tsuyoshi,Ohtani, Akio
experimental part, p. 546 - 548 (2010/04/26)
We describe in this Letter a new synthetic method for pyrrolin-2-ones as potent plasminogen activator inhibitor-1 (PAI-1) inhibitors. Pyrrolin-2-one derivatives synthesized from N-2-oxoethylamides and aldehydes in aqueous NaOH by one-pot were evaluated for their PAI-1 inhibitory activity. Among these derivatives, compounds 16 and 18 were found to possess potent PAI-1 inhibitory activity (compound 16: IC50: 0.69 μM, compound 18: IC50: 0.65 μM).