Nazaré Marc, Essrich Melanie, Will David W, Matter Hans, Ritter Kurt, Urmann Matthias, Bauer Armin, Schreuder Herman, Dudda Angela, Czech Jörg, Lorenz Martin, Laux Volker, Wehner Volkmar
Aventis Pharma Deutschland GmbH, D-65926 Frankfurt am Main, Germany.
Bioorg Med Chem Lett. 2004 Aug 16;14(16):4191-5. doi: 10.1016/j.bmcl.2004.06.020.
A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for neutral ligands, which bind in the S1 pocket of factor Xa were investigated with the 2-carboxyindole scaffold. This privileged fragment assembly approach yielded a set of equipotent, selective inhibitors with structurally diverse neutral P1 substituents.
描述了一系列新型、高效的基于2-羧基吲哚的凝血因子Xa抑制剂。利用2-羧基吲哚骨架研究了结合在凝血因子Xa的S1口袋中的中性配体的结构要求。这种独特的片段组装方法产生了一组具有结构多样的中性P1取代基的等效、选择性抑制剂。
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