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Phenyltriazolinones as potent factor Xa inhibitors |
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| Authors: | Mimi L Quan Donald JP Pinto Karen A Rossi Steven Sheriff Richard S Alexander Eugene Amparo Kevin Kish Robert M Knabb Joseph M Luettgen Paul Morin Angela Smallwood Francis J Woerner Ruth R Wexler |
| Institution: | Research and Development, Bristol-Myers Squibb, PO Box 5400, Princeton, NJ 08543-5400, United States |
| Abstract: | We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the phenyltriazolinone P1 substrate. |
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