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Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs |
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| Authors: | Young Robert J Borthwick Alan D Brown David Burns-Kurtis Cynthia L Campbell Matthew Chan Chuen Charbaut Marie Chung Chun-wa Convery Máire A Kelly Henry A Paul King N Kleanthous Savvas Mason Andrew M Pateman Anthony J Patikis Angela N Pinto Ivan L Pollard Derek R Senger Stefan Shah Gita P Toomey John R Watson Nigel S Weston Helen E |
| Institution: | GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. Rob.J.Young@gsk.com |
| Abstract: | Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl P4 groups, producing highly potent inhibitors with encouraging oral pharmacokinetic profiles and significant but sub-optimal anticoagulant activities. |
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