Opening the piperazine ring of M55113 and M55551 to an ethylenediamine structure significantly reduces Factor Xa inhibitory activity.
Piperazine ring opening markedly reduces FXa inhibition in these analogs; leaves open whether alternative modifications merit further preclinical SAR studies.
Compounds containing an ethylenediamine structure in place of the piperazine ring of M55113 (1) and M55551 (2) were synthesized to investigate the effects of a piperazine moiety and evaluated for activity as factor Xa (FXa) inhibitors. Most such compounds, however, exhibited lower activity (1/10-1/100) than that of M55113 and M55551 as FXa inhibitors.
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Nishida et al. (2004) studied this question.
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