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  • Title: Phenyltriazolinones as potent factor Xa inhibitors.
    Author: Quan ML, Pinto DJ, Rossi KA, Sheriff S, Alexander RS, Amparo E, Kish K, Knabb RM, Luettgen JM, Morin P, Smallwood A, Woerner FJ, Wexler RR.
    Journal: Bioorg Med Chem Lett; 2010 Feb 15; 20(4):1373-7. PubMed ID: 20100660.
    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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