Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa.
The serine protease factor Xa is a critical enzyme in the blood coagulation cascade. Recently, the inhibition of factor Xa has begun to emerge as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe a series of meta-amidino-N,N-disubstituted anilines as structurally simple and very potent inhibitors of factor Xa.
Fevig
J M
JM
DuPont Pharmaceuticals Company, Wilmington, DE 19880-0500, USA.
Cacciola
J
J
Alexander
R S
RS
Knabb
R M
RM
Lam
G N
GN
Wong
P C
PC
Wexler
R R
RR
D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D011817:Rabbits; D013329:Structure-Activity Relationship
D000814:Aniline Compounds; D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents