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Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.

Abstract：

:In an effort to identify a potential back-up to apixaban (Eliquis®), we explored a series of diversified P4 moieties. Several analogs with substituted gem-dimethyl moieties replacing the terminal lactam of apixaban were identified which demonstrated potent FXa binding affinity (FXa Ki), good human plasma anticoagulant activity (PT EC2x), cell permeability, and oral bioavailability.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Orwat MJ,Qiao JX,He K,Rendina AR,Luettgen JM,Rossi KA,Xin B,Knabb RM,Wexler RR,Lam PY,Pinto DJ

doi

10.1016/j.bmcl.2014.05.101

subject

Has Abstract

pub_date

2014-08-01 00:00:00

pages

3341-5

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00610-6

journal_volume

24

pub_type

杂志文章

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