Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. Part 6: further focus on the contracted C4'-side chain analogues.
Novel benzo[b]thiophene diamine thrombin inhibitors were investigated, focusing on a contracted C4'-side chain series. SAR studies identified compounds with either a pyrrolidino or morpholino group as potent, active site directed thrombin inhibitors when the amino group was connected to the C3-phenyl ring with a methylene linker at the C4' position of the phenyl ring.
Takeuchi
K
K
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. ktak@lilly.com
Kohn
T J
TJ
Harper
R W
RW
Lin
H S
HS
Gifford-Moore
D S
DS
Richett
M E
ME
Sall
D J
DJ
Smith
G F
GF
Zhang
M
M
D000991:Antithrombins / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry* / Q000494:pharmacology*
D000991:Antithrombins; D013876:Thiophenes; C088015:benzothiophene