Title of article
Selective and dual action orally active inhibitors of thrombin and factor Xa
Author/Authors
Robert J. Young، نويسنده , , David Brown، نويسنده , , Cynthia L. Burns-Kurtis، نويسنده , , Chuen Chan، نويسنده , , M?ire A. Convery، نويسنده , , Julia A. Hubbard، نويسنده , , Henry A. Kelly، نويسنده , , Anthony J. Pateman، نويسنده , , Angela Patikis، نويسنده , , Stefan Senger، نويسنده , , Gita P. Shah، نويسنده , , John R. Toomey، نويسنده , , Nigel S. Watson، نويسنده , , Ping Zhou، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
2927
To page
2930
Abstract
The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. This was achieved through minor modifications to the sulfonamide group in our potent and selective fXa inhibitor (E)-2-(5-chlorothien-2-yl)-N-{(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl}ethenesulfonamide and these observed activity changes have been rationalised using structural studies.
Keywords
Factor Xa , oral , Dual Inhibitor , thrombin
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798151
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