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Selective and dual action orally active inhibitors of thrombin and factor Xa |
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| Authors: | Young Robert J Brown David Burns-Kurtis Cynthia L Chan Chuen Convery Máire A Hubbard Julia A Kelly Henry A Pateman Anthony J Patikis Angela Senger Stefan Shah Gita P Toomey John R Watson Nigel S Zhou Ping |
| Institution: | GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. Rob.J.Young@gsk.com |
| 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. |
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