229647-15-8Relevant articles and documents
Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor
Nishida,Miyazaki,Kitamura,Ohashi,Matsusue,Okamoto,Hosaka,Ohnishi,Mochizuki
, p. 1237 - 1244 (2007/10/03)
Intravascular clot formation is an important factor in a number of cardiovascular diseases. Therefore, the prevention of blood coagulation has become a major target for new therapeutic agents. One attractive approach is the inhibition of factor Xa (FXa), which is a key enzyme in coagulation cascade responsible for the generation of thrombin by limited proteolysis of its zymogen, prothrombin. We have investigated 1-arylsulfonyl-3-piperazinone derivatives, containing a 4-(piperidino)pyridine group in place of guanidino and/or amidino groups, and discovered compound M55113 (30a: 4-[(6-Chloro-2-naphthalenyl)sulfonyl]-1-[[1-(4-pyridinyl)-4-piperidinyl]- methyl]piperazinone), as a potent inhibitor of FXa (IC50=0.06 μM) with high selectivity for FXa over trypsin and thrombin.