Macrocyclic factor XIa inhibitors.

Abstract:

: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.

journal_name

Bioorg Med Chem Lett

authors

Wang C,Corte JR,Rossi KA,Bozarth JM,Wu Y,Sheriff S,Myers JE Jr,Luettgen JM,Seiffert DA,Wexler RR,Quan ML

doi

10.1016/j.bmcl.2017.07.048

subject

Has Abstract

pub_date

2017-09-01 00:00:00

pages

4056-4060

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(17)30755-2

journal_volume

27

pub_type

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