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Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor

H Nishida1, Y Miyazaki, Y Kitamura

  • 1Chemistry Laboratory, Research Center, Mochida Pharmaceutical Co., Ltd., Gotemba, Shizuoka, Japan. hnishida@mochida.co.jp

Chemical & Pharmaceutical Bulletin
|October 19, 2001
PubMed

Insights

Researchers identified a new compound, M55113, that potently inhibits factor Xa (FXa), a key enzyme in blood clot formation. This discovery offers a promising avenue for developing new anticoagulant therapies to prevent cardiovascular diseases.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Biochemistry

Background:

  • Intravascular clot formation contributes to cardiovascular diseases.
  • Preventing blood coagulation is a therapeutic target for cardiovascular conditions.
  • Factor Xa (FXa) is a critical enzyme in the coagulation cascade, essential for thrombin generation.

Purpose of the Study:

  • To investigate novel 1-arylsulfonyl-3-piperazinone derivatives as potential anticoagulant agents.
  • To identify potent and selective inhibitors of factor Xa (FXa).

Main Methods:

  • Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives.
  • Assay of inhibitory activity against factor Xa (FXa).
  • Assessment of selectivity against related enzymes like trypsin and thrombin.

Main Results:

  • Compound M55113 (30a) was identified as a potent inhibitor of factor Xa (FXa).
  • M55113 demonstrated significant inhibitory activity with an IC50 of 0.06 microM.
  • The compound exhibited high selectivity for FXa over trypsin and thrombin.

Conclusions:

  • Compound M55113 is a potent and selective inhibitor of factor Xa (FXa).
  • This derivative represents a promising lead compound for the development of new anticoagulant drugs.
  • Targeting FXa offers a viable strategy for managing thrombotic disorders.

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