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.
A facile and simple method for the reduction of N-protected amino acids and peptides to the corresponding alcohols
A practical and chemoselective method for the reduction of N-protected amino acids and peptides including carboxylic acids to their corresponding alcohols is outlined.
Srivastava, Tumul,Srivastava, Tushar K.,Haq,Katti, Seturam B.
p. 516 - 517
(2007/10/03)
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.
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(2008/06/13)
An efficient method for the reduction of N-protected amino acids and peptides to the corresponding alcohols
Reduction of pentachlorophenyl esters of Boc protected amino acids and peptides to the corresponding alcohols is described.
Naqvi,Bhattacharya,Haq
p. 424 - 425
(2007/10/03)
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