Synthesis And Evaluation Of 1-Arylsulfonyl-3-Piperazinone Derivatives As Factor Xa Inhibitors Vi. A Series Of New Derivatives Containing N,S- And N,So2-Spiro Acetal Scaffolds

CHEMICAL & PHARMACEUTICAL BULLETIN(2007)

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摘要
In the course of development of factor Xa (FXa) inhibitors, we have found unique compounds containing an N,O- and an NA-spiro acetal structure. It appeared that the difference in overall conformation due to the N,Y-spiro acetal structure might be important for FXa inhibitory activity. Therefore, other NA-spiro acetal structures, an NS- and an NSO2-spiro acetal, were developed as analogues of the N,X-spiro acetal structure. Compound 7b (N,S-spiro acetal structure) was found to have the strongest activity in these series of N,X-spiro acetal compounds, which had ever been synthesized.(4,5))
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关键词
factor Xa inhibitor, structure-activity relationship, N,S-spiro acetal, N,SO2-spiro acetal, intramolecular cyclization
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