58266-36-7Relevant academic research and scientific papers
Synthesis and evaluation of 1,4-diphenylbutadiene derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) production
Miyazaki, Hiroshi,Sai, Hiroshi,Ohmizu, Hiroshi,Murakami, Jun,Ohtani, Akio,Ogiku, Tsuyoshi
experimental part, p. 1968 - 1979 (2010/05/18)
Butadiene-imide 1 (T-686) derivatives were synthesized and evaluated for their inhibitory activity against PAI-1 production and their ADMET (DMPK and toxicology) profiles. Among these derivatives, compound 15k (T-2639) showed good antithrombotic activity in two rat thrombosis models without affecting bleeding time, indicating reduction of haemorrhagic risk. We also describe in this report a practical synthesis of 15k suitable for scale-up using Z,E-selective Stobbe condensation.
Design, synthesis, and evaluation of orally active inhibitors of plasminogen activator inhibitor-1 (PAI-1) production
Miyazaki, Hiroshi,Ogiku, Tsuyoshi,Sai, Hiroshi,Ohmizu, Hiroshi,Murakami, Jun,Ohtani, Akio
scheme or table, p. 6419 - 6422 (2009/09/06)
A novel series of butadiene-imide 1 (T-686) derivatives having an inhibitory activity against PAI-1 production was synthesized and evaluated their biological activities and DMPK profiles, in which 15k (T-2639) was selected as the best compound based on its strong antithrombotic activity and good bioavailability.
