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 Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Wang C,Corte JR,Rossi KA,Bozarth JM,Wu Y,Sheriff S,Myers JE Jr,Luettgen JM,Seiffert DA,Wexler RR,Quan MLdoi
10.1016/j.bmcl.2017.07.048subject
Has Abstractpub_date
2017-09-01 00:00:00pages
4056-4060issue
17eissn
0960-894Xissn
1464-3405pii
S0960-894X(17)30755-2journal_volume
27pub_type
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