Selective and dual action orally active inhibitors of thrombin and factor Xa.
Bioorg Med Chem Lett
; 17(10): 2927-30, 2007 May 15.
Article
in En
| MEDLINE
| ID: mdl-17420122
ABSTRACT
The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. This was achieved through minor modifications to the sulfonamide group in our potent and selective fXa inhibitor (E)-2-(5-chlorothien-2-yl)-N-{(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl}ethenesulfonamide and these observed activity changes have been rationalised using structural studies.
Search on Google
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Sulfonamides
/
Thrombin
/
Morpholines
/
Fibrinolytic Agents
/
Factor Xa Inhibitors
Type of study:
Prognostic_studies
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2007
Type:
Article
Affiliation country:
United kingdom