Compound 7b, an N,S-spiro acetal derivative, demonstrated potent Factor Xa inhibitory activity in vitro, suggesting potential as a novel anticoagulant scaffold.
7b merits preclinical testing as FXa inhibitor lead; leaves open in vivo efficacy and clinical translation.
In the course of development of factor Xa (FXa) inhibitors, we have found unique compounds containing an N,O- and an N,N-spiro acetal structure. It appeared that the difference in overall conformation due to the N,X-spiro acetal structure might be important for FXa inhibitory activity. Therefore, other N,X-spiro acetal structures, an N,S- and an N,SO2-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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Saitoh et al. (2007) studied this question.
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