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Issue 2, 2014
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Transformation of a selective factor Xa inhibitor rivaroxaban into a dual factor Xa/thrombin inhibitor by modification of the morpholin-3-one moiety

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Abstract

Replacement of the P4 morpholin-3-one moiety in a selective factor Xa inhibitor rivaroxaban by 2-ethoxycarbonylpiperidine resulted in a dual factor Xa/thrombin inhibitor 24, possessing a Ki of 62 ± 18 nM for factor Xa and a Ki of 353 ± 75 nM for thrombin. Presented rationalization of dual activity provides a good starting point for “designing in” thrombin inhibitory activity to potent factor Xa inhibitor rivaroxaban.

Graphical abstract: Transformation of a selective factor Xa inhibitor rivaroxaban into a dual factor Xa/thrombin inhibitor by modification of the morpholin-3-one moiety

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Supplementary files

Article information


Submitted
03 Sep 2013
Accepted
29 Nov 2013
First published
04 Dec 2013

Med. Chem. Commun., 2014,5, 197-202
Article type
Concise Article

Transformation of a selective factor Xa inhibitor rivaroxaban into a dual factor Xa/thrombin inhibitor by modification of the morpholin-3-one moiety

U. Trstenjak, J. Ilaš and D. Kikelj, Med. Chem. Commun., 2014, 5, 197
DOI: 10.1039/C3MD00250K

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