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ID: ALA1136021
Journal: Bioorg Med Chem Lett
Title: Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.
Authors: Song Y, Clizbe L, Bhakta C, Teng W, Li W, Wu Y, Jia ZJ, Zhang P, Wang L, Doughan B, Su T, Kanter J, Woolfrey J, Wong P, Huang B, Tran K, Sinha U, Park G, Reed A, Malinowski J, Hollenbach S, Scarborough RM, Zhu BY.
Abstract: Substituted acrylamides were used as templates that bridge P1 and P4 binding elements, resulting in a series of potent (sub-nanomolar) and selective factor Xa inhibitors. In this template, cis-geometry of P1 and P4 ligands is highly preferred. SAR on the substituting groups, as well as on modification of P1 and P4 moieties is described. Compounds in this series show good in vivo efficacy in animal models.
CiteXplore: 12031331