The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.
Bioorg Med Chem Lett
; 21(6): 1588-92, 2011 Mar 15.
Article
in En
| MEDLINE
| ID: mdl-21349711
ABSTRACT
The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the former series were addressed in the later, delivering a robust candidate for progression towards clinical studies.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Benzazepines
/
Serine Proteinase Inhibitors
/
Tetrahydroisoquinolines
/
Factor Xa Inhibitors
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2011
Type:
Article
Affiliation country:
United kingdom