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Investigation of factor Xa inhibitors containing non-amidine S1 elements
Authors:Franciskovich Jeffry B  Masters John J  Tinsley Jennifer M  Craft Trelia J  Froelich Larry L  Gifford-Moore Donetta S  Klimkowski Valentine J  Smallwood Jeffrey K  Smith Gerald F  Smith Tommy  Towner Richard R  Weir Leonard C  Wiley Michael R
Institution:Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. j.franciskovich@lilly.com
Abstract:Several non-amidino S1 derivatives of the 1,2-diaminobenzene-based scaffold (4) were synthesized and evaluated for their ability to bind to the active site and inhibit the human protease factor Xa. A subset of these compounds were also evaluated for their anticoagulant effects in human plasma as measured by prothrombin time (PT).
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