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ID: ALA1144307

Journal: Bioorg Med Chem Lett

Title: Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.

Authors: Groebke Zbinden K, Banner DW, Ackermann J, D'Arcy A, Kirchhofer D, Ji YH, Tschopp TB, Wallbaum S, Weber L.

Abstract: Proof of concept experiments have shown that tissue factor/factor VIIa inhibitors have antithrombotic activity without enhancing bleeding propensity. Starting from lead compounds generated by a biased combinatorial approach, phenylglycine amide tissue factor/factor VIIa inhibitors with low nanomolar affinity and good selectivity against other serine proteases of the coagulation cascade were designed, using the guidance of X-ray structural analysis and molecular modelling.

CiteXplore: 15664864

DOI: 10.1016/j.bmcl.2004.10.092