138971-64-9

Upstream product

• 143646-44-0 2-Benzyloxycarbonylamino-3,3-diphenyl-propionic acid 2,5-dioxo-pyrrolidin-1-yl ester 
• 147-85-3 L-proline 
• 776-74-9 Bromodiphenylmethane 
• 143646-43-9 ethyl acetamido(diphenylmethyl)cyanoacetate 
• 119273-60-8 2-amino-3,3-diphenylpropanoic acid hydrochloride 
• 143218-09-1 2-Benzyloxycarbonylamino-3,3-diphenyl-propionic acid 
• 13139-17-8 N-(Benzyloxycarbonyloxy)succinimide 

Downstream Products

• 195515-90-3 2-{[(S)-1-((R)-2-Benzyloxycarbonylamino-3,3-diphenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-2-hydroxymethyl-3-phenyl-propionic acid 
• 252731-93-4 Z-D-Dpa-Pro-NHMpGly^P(OPh)2 
• 143729-52-6 Z-D-Dpa-Pro-NHPGly^P(OPh)2 
• 161442-06-4 (1-{[(S)-1-((R)-2-Amino-3,3-diphenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-4-methoxy-butyl)-phosphonic acid diphenyl ester 
• 143729-53-7 (1-{[(S)-1-((R)-2-Amino-3,3-diphenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-hexyl)-phosphonic acid diphenyl ester 
• 143729-54-8 (1-{[(S)-1-((R)-2-Amino-3,3-diphenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-hexyl)-phosphonic acid 
• 143217-75-8 (S)-1-((R)-2-Amino-3,3-diphenyl-propionyl)-pyrrolidine-2-carboxylic acid [1-(3-guanidino-propyl)-2,5-dioxo-5-piperidin-1-yl-pentyl]-amide; compound with trifluoro-acetic acid 
• 143217-99-6 C₅₂H₆₅N₇O₉S 
• 143217-93-0 C₄₈H₅₈N₆O₁₀S 
• 143217-82-7 C₄₄H₅₂N₆O₉S 
• 195515-91-4 2-(2-{[(S)-1-((R)-2-Benzyloxycarbonylamino-3,3-diphenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-2-hydroxymethyl-3-phenyl-propionylamino)-benzoic acid benzyl ester 
• 195515-92-5 2-(2-{[(S)-1-((R)-2-Amino-3,3-diphenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-2-hydroxymethyl-3-phenyl-propionylamino)-benzoic acid 
• 195515-94-7 2'-({[(S)-1-((R)-2-Amino-3,3-diphenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-methyl)-biphenyl-2-carboxylic acid 
• 195515-93-6 2'-({[(S)-1-((R)-2-Benzyloxycarbonylamino-3,3-diphenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-methyl)-biphenyl-2-carboxylic acid 

Relevant academic research and scientific papers

Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors

Ketomethylene pseudopeptide analogues Aa-Pro-Argψ(COCH2)Gly-pip, 1, where Aa are D- or L-amino acids (Dpa, β,β-diphenylalanine; αNal, α- naphthylalanine; βNal, β-naphthylalanine; Fgl, fluorenylglycine) with highly lipophilic side chains and ψ(COCH2) is a ketomethylene pseudopeptide bond, have been synthesized through a modified Dakin-West reaction under very mild conditions with a high yield using tripeptide 4 with a labile functional group directly on the side chain. Their enzymatic assay of thrombin inhibition has been carried out. The structure-activity relationship study indicated that a lipophilic side chain on the amino acid in the P3 position is very important for binding to the apolar site of thrombin. Compound 1a with D-Dpa at the P3 position has a K(i) of 0.2 μM and it doubles thrombin clotting time at only 3 times higher concentration. These values are about 7 times better than those of the corresponding D-Phe analogues. Furthermore, 1a shows poor inhibitory activity against plasmin, factor Xa, urokinase, and kallikrein. Preliminary in vivo testing (3-4-kg rabbit as the animal model) shows no observable side effect (change of blood pressure and accumulation of blood platelet in lungs) at a dose of 1 mg/kg.