Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability

[Display omitted] This manuscript describes the discovery of a series of macrocyclic inhibitors of FXIa with oral bioavailability. Assisted by structure based drug design and ligand bound X-ray crystal structures, the group linking the P1 moiety to the macrocyclic core was modified with the goal of...

Ausführliche Beschreibung

Bibliographische Detailangaben

Veröffentlicht in:	Bioorg. Med. Chem. Lett 2019-10, Vol.29 (19), p.126604-126604, Article 126604
Hauptverfasser:	Clark, Charles G., Rossi, Karen A., Corte, James R., Fang, Tianan, Smallheer, Joanne M., De Lucca, Indawati, Nirschl, David S., Orwat, Michael J., Pinto, Donald J.P., Hu, Zilun, Wang, Yufeng, Yang, Wu, Jeon, Yoon, Ewing, William R., Myers, Joseph E., Sheriff, Steven, Lou, Zhen, Bozarth, Jeffrey M., Wu, Yiming, Rendina, Alan, Harper, Timothy, Zheng, Joanna, Xin, Baomin, Xiang, Qian, Luettgen, Joseph M., Seiffert, Dietmar A., Wexler, Ruth R., Lam, Patrick Y.S.
Format:	Artikel
Sprache:	eng
Schlagworte:	Activated partial thromboplastin time Anticoagulant aPTT Bioavailability Factor XIa inhibitors FXIa Thrombosis
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!