2d1j: Difference between revisions

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==Overview==
==Overview==
Compound 7 was identified as the active metabolite of 6 by HPLC and mass, spectral analysis. Modification of lead compound 7 by transformation of, its N-oxide 6-6 biaryl ring system and fused aromatics produced a series, of non-basic fXa inhibitors with excellent potency in anti-fXa and, anticoagulant assays. The optimized compounds 73b and 75b showed sub to, one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa activity was detected in plasma of rats orally administered with, 1mg/kg of compound 75b.
Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral analysis. Modification of lead compound 7 by transformation of its N-oxide 6-6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays. The optimized compounds 73b and 75b showed sub to one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa activity was detected in plasma of rats orally administered with 1mg/kg of compound 75b.


==Disease==
==Disease==
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[[Category: serine protease]]
[[Category: serine protease]]


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