Title of article :
Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an α-ketothiazole arginine
Author/Authors :
Hongfeng Deng، نويسنده , , Thomas D. Bannister، نويسنده , , Lei Jin، نويسنده , , Robert E. Babine، نويسنده , , Jesse Quinn، نويسنده , , Pamela Nagafuji، نويسنده , , Cassandra A. Celatka، نويسنده , , Jian Lin، نويسنده , , Tsvetelina I. Lazarova، نويسنده , , Michael J. Rynkiewicz، نويسنده , , Frank Bibbins، نويسنده , , Pramod Pandey، نويسنده , , Joan Gorga، نويسنده , , Harold V. Meyers، نويسنده , , Sherin S. Abdel-Meguid، نويسنده , , James E. Strickler، نويسنده ,
Abstract :
Using an α-ketothiazole arginine moiety as a key recognition element, a series of small peptidomimetic molecules was designed and synthesized, and their co-crystal structures with factor XIa were studied in an effort to develop smaller, less peptidic inhibitors as antithrombotic agents.
Keywords :
Factor XIa inhibitor , ?-Ketothiazole arginine , X-ray crystal structure , Anticoagulant