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4-{[(E)-2-(5-CHLOROTHIEN-2-YL)VINYL]SULFONYL}-1-(1H-PYRROLO[3,2-C]PYRIDIN-2-YLMETHYL)PIPERAZIN-2-ONE
- Development stage
- Preclinical
- Lead developer
- Sanofi
- Modality
- Small Molecules
01
Overview
This compound is a synthetic small molecule inhibitor of human coagulation factor Xa. It features a sulfonyl-keto piperazine scaffold and was developed as part of research into non-peptide inhibitors targeting the S1 pocket of factor Xa. The molecule binds in a unique "reverse" mode to the active site of factor Xa, forming key hydrogen bonds and exploiting both neutral and basic substituents for selectivity. Its primary mechanism is inhibition of serine protease activity in the coagulation cascade by directly binding to factor Xa. The compound has been studied experimentally but has not advanced beyond preclinical or early-phase development for anticoagulation indications.[5]
- Other names
- 4-{[(E)-2-(5-chlorothien-2-yl)vinyl]sulfonyl}-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)piperazin-2-one4-{[(E)-2-(5-chlorothiophen-2-yl)ethenyl]sulfonyl}-1-(1H-pyrrolo[3,2-c]pyridin-2-yImethyl)piperazinone4-[[(E)-2-(5-chlorothiophen-2-yI)etheneyl]sulfonyl]-1-[{IH-pyrrolo[3, 20c}pyridin - 20yImethyl}piperazin - 20one
02
Targets
F10 (Factor Xa)
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