Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker

A novel series of macrocyclic FXIa inhibitors was designed based on our lead acyclic phenyl imidazole chemotype. Our initial macrocycles, which were double-digit nanomolar FXIa inhibitors, were further optimized with assistance from utilization of structure-based drug design and ligand bound X-ray c...

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Veröffentlicht in:	Journal of medicinal chemistry 2017-02, Vol.60 (3), p.1060-1075
Hauptverfasser:	Corte, James R, Fang, Tianan, Osuna, Honey, Pinto, Donald J. P, Rossi, Karen A, Myers, Joseph E, Sheriff, Steven, Lou, Zhen, Zheng, Joanna J, Harper, Timothy W, Bozarth, Jeffrey M, Wu, Yiming, Luettgen, Joseph M, Seiffert, Dietmar A, Decicco, Carl P, Wexler, Ruth R, Quan, Mimi L
Format:	Artikel
Sprache:	eng
Schlagworte:	activated partial thromboplastin time amides Amides - chemistry anticoagulant antithrombotic aPTT Drug Discovery factor XIa Factor XIa - antagonists & inhibitors factor XIa inhibitors FXIa FXIa inhibitors Hydrogen Bonding inhibitors INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY Ligands macrocycles Macrocyclic Compounds - chemistry Macrocyclic Compounds - pharmacokinetics Macrocyclic Compounds - pharmacology Molecular Structure peptides and proteins phenyls Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - pharmacokinetics Serine Proteinase Inhibitors - pharmacology thrombosis
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