Synthesis and Evaluation of 1-Arylsulfonyl-3-piperazinone Derivatives as Factor Xa Inhibitor.
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- NISHIDA Hidemitsu
- Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd.
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- MiYAZAKI Yutaka
- Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd.
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- KITAMURA Yoshihiro
- Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd.
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- OHASHI Masayuki
- Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd.
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- MATSUSUE Tomokazu
- Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd.
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- OKAMOTO Atsushi
- Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd.
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- HOSAKA Yoshitaka
- Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd.
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- OHNISHI Shuhei
- Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd.
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- MOCHIZUKI Hidenori
- Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd.
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Description
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.
Journal
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- Chemical and Pharmaceutical Bulletin
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Chemical and Pharmaceutical Bulletin 49 (10), 1237-1244, 2001
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390001204164043392
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- NII Article ID
- 110003615768
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- NII Book ID
- AA00602100
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- COI
- 1:CAS:528:DC%2BD3MXnt1Cksb0%3D
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- ISSN
- 13475223
- 00092363
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- NDL BIB ID
- 5926517
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- PubMed
- 11605647
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed