342908-14-9

Upstream product

• 244257-59-8 (4R)-4-t-butoxycarbonylamino-5-chloropentanoic acid benzyl ester 
• 210962-75-7 3-hydroxy-4-iodobenzonitrile 
• 195434-34-5 (4R)-4-t-butoxycarbonylamino-5-hydroxypentanoic acid benzyl ester 
• 35793-73-8 N-(tert-butyloxycarbonyl)-γ-benzyl-D-glutamic acid 
• 342908-13-8 (4R)-4-t-butoxycarbonylamino-5-(methanesulfonyloxy)pentanoic acid benzyl ester 

Relevant academic research and scientific papers

Optimization of a coagulation factor VIIa inhibitor found in factor Xa inhibitor library

An inhibitor of the complex of factor VIIa and tissue factor (fVIIa/TF), 2-substituted-4-amidinophenylpyruvic acid 1a, was structurally modified with the aim of increasing its potency and selectivity. The lead compound 1a was originally found in our factor Xa (fXa) inhibitor library on the basis of structural similarity of the primary binding sites of fVIIa and fXa. The design was based on computational docking studies using the extracted active site of fVIIa. Compound 1j was found to inhibit factor VIIa/TF at nanomolar concentration with improved selectivity versus fXa and thrombin and it preferentially prolonged the clotting time in the TF-dependent extrinsic pathway.

AMIDINOPHENYLPYRUVIC ACID DERIVATIVES

An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.