ChemInform Abstract: Synthesis and Evaluation of 1-Arylsulfonyl-3-piperazinone Derivatives as Factor Xa Inhibitor

Autor:	Hidemitsu Nishida, Yutaka Miyazaki, Masayuki Ohashi, Atsushi Okamoto, Yoshitaka Hosaka, Yoshihiro Kitamura, Hidenori Mochizuki, Tomokazu Matsusue, Shuhei Ohnishi
Rok vydání:	2010
Předmět:	Sulfonyl chemistry.chemical_classification medicine.drug_mechanism_of_action medicine.diagnostic_test Chemistry Stereochemistry Proteolysis Factor Xa Inhibitor General Medicine Trypsin Thrombin Coagulation Zymogen medicine IC50 medicine.drug
Zdroj:	ChemInform. 33
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200212265
Popis:	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.
Databáze:	OpenAIRE
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