Macrocyclic factor XIa inhibitors

DOI: 10.1016/j.bmcl.2017.07.048

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 4056 - 4060 (2017)

Update date:2022-08-05

Topics:

Authors:

Wang, Cailan

Corte, James R.

Rossi, Karen A.

Bozarth, Jeffrey M.

Wu, Yiming

Sheriff, Steven

Myers, Joseph E.

Luettgen, Joseph M.

Seiffert, Dietmar A.

Wexler, Ruth R.

Quan, Mimi L.

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Article abstract of DOI:10.1016/j.bmcl.2017.07.048

A series of macrocyclic factor XIa (FXIa) inhibitors was designed based on an analysis of the crystal structures of the acyclic phenylimidazole compounds. Further optimization using structure-based design led to inhibitors with pM affinity for FXIa, excellent selectivity against a panel of relevant serine proteases, and good potency in the activated partial thromboplastin time (aPTT) clotting assay.

Full text of DOI:10.1016/j.bmcl.2017.07.048

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