Thrombin inhibitors based on a propargylglycine template.
A series of novel arylsulfonylpropargylglycinamide derivatives was investigated as thrombin inhibitors in which the SAR was focused on substituents at the acetylenic terminus. Several compounds in this series were identified as potent thrombin inhibitors (Ki up to 5 nM) that are highly selective over trypsin and other serine proteases as well.
Lee
K
K
Biotech Research Institute, LG Chemical Ltd/Research Park, Yu Sung Science Town, Taejon, Korea.
Hwang
S Y
SY
Park
C W
CW
D000480:Alkynes / Q000737:chemistry*; D000818:Animals; D000991:Antithrombins / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D019540:Area Under Curve; D005998:Glycine / Q000031:analogs & derivatives* / Q000737:chemistry; D051381:Rats; D013329:Structure-Activity Relationship
D000480:Alkynes; D000991:Antithrombins; C009055:propargylglycine; D005998:Glycine