197979-64-9Relevant 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.
Practical synthetic method of (2Z,3E)-1,4-Diphenylbutadiene T-2639, an inhibitor of plasminogen activator inhibitor-1 (PAI-1) production
Miyazaki, Hiroshi,Ohmizu, Hiroshi,Ogiku, Tsuyoshi
body text, p. 760 - 763 (2010/04/22)
A practical synthetic method of (2Z,3E)-1,4-diphenylbutadiene derivative T-2369 (1), a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1) production, is described. Conditions of Stobbe condensation in the conventional synthesis of T-2369 were e
