5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.
Syntheses and SAR studies of 5-amidinobenzo[b]thiophene analogs provided compounds with low submicromolar factor IXa activity and equal or slightly better selectivity relative to factor Xa.
Qiao
Jennifer X
JX
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. jennifer.qiao@bms.com
Cheng
Xuhong
X
Modi
Dilip P
DP
Rossi
Karen A
KA
Luettgen
Joseph M
JM
Knabb
Robert M
RM
Jadhav
Prabhakar K
PK
Wexler
Ruth R
RR
D015949:Factor IXa / Q000037:antagonists & inhibitors*; D065427:Factor Xa Inhibitors; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology*
D065427:Factor Xa Inhibitors; D015842:Serine Proteinase Inhibitors; D013876:Thiophenes; D015949:Factor IXa