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  • Title: Investigation of the terminal P4 domain in a series of D-phenylglycinamide-based factor Xa inhibitors.
    Author: Franciskovich JB, Masters JJ, Weber WW, Klimkowski VJ, Chouinard M, Sipes PR, Johnson LM, Snyder DW, Chastain MK, Craft TJ, Towner RD, Gifford-Moore DS, Froelich LL, Smallwood JK, Foster RS, Smith GF, Liebeschuetz JW, Murray CW, Young SC.
    Journal: Bioorg Med Chem Lett; 2007 Dec 15; 17(24):6910-3. PubMed ID: 17976987.
    Abstract:
    Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant effects in vitro. A select subset containing various P1 indole constructs was further evaluated for their pharmacokinetic properties after oral administration to rats.
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