760214-59-3

Upstream product

• 77119-85-8 N-(tert-butoxycarbonyl)-D-phenylalaninal 
• 21204-67-1 methyl (triphenylphosphoranylidene)acetate 
• 18942-49-9 Boc-D-Phe-OH 
• 760214-60-6 (R,E)-4-((tert-butoxycarbonyl)amino)-5-phenylpent-2-enoic acid 
• 19901-50-9 methyl (2R)-2-(t-butoxycarbonylamino)-3-phenylpropionate 

Downstream Products

• 213126-02-4 (E)-(R)-4-[3-(2-Iodo-phenyl)-ureido]-5-phenyl-pent-2-enoic acid methyl ester 
• 213126-17-1 (E)-(R)-4-[3-Benzyl-3-(2-iodo-phenyl)-ureido]-5-phenyl-pent-2-enoic acid methyl ester 
• 213126-44-4 1-[(E)-(R)-1-Benzyl-4-(tert-butyl-dimethyl-silanyloxy)-but-2-enyl]-3-(2-iodo-phenyl)-urea 
• 760214-64-0 {3-[(E)-(R)-4-(3-biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoylamino]-propyl}-carbamic acid tert-butyl ester 
• 760214-62-8 {2-[(E)-(R)-4-(3-biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoylamino]-ethyl}-carbamic acid tert-butyl ester 
• 760214-73-1 [(E)-(R)-1-benzyl-3-(2-pyrrolidin-1-yl-ethylcarbamoyl)-allyl]-carbamic acid tert-butyl ester 
• 760214-61-7 (E)-(R)-4-(3-biphenyl-4-yl-ureido)-5-phenyl-pent-2-enoic acid 
• 760214-60-6 (R,E)-4-((tert-butoxycarbonyl)amino)-5-phenylpent-2-enoic acid 

Relevant academic research and scientific papers

Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and Trypanosoma cruzi Cruzain

Gallinamide A, originally isolated with a modest antimalarial activity, was subsequently reisolated and characterized as a potent, selective, and irreversible inhibitor of the human cysteine protease cathepsin L. Molecular docking identified potential modifications to improve binding, which were synthesized as a suite of analogs. Resultingly, this current study produced the most potent gallinamide analog yet tested against cathepsin L (10, Ki = 0.0937 ± 0.01 nM and kinact/Ki = 8 730 000). From a protein structure and substrate preference perspective, cruzain, an essential Trypanosoma cruzi cysteine protease, is highly homologous. Our investigations revealed that gallinamide and its analogs potently inhibit cruzain and are exquisitely toxic toward T. cruzi in the intracellular amastigote stage. The most active compound, 5, had an IC50 = 5.1 ± 1.4 nM, but was relatively inactive to both the epimastigote (insect stage) and the host cell, and thus represents a new candidate for the treatment of Chagas disease.

CARBAMOYL PHENYLALANINOL ANALOGS AND USES THEREOF

The present invention relates to carbamoyl phenylalaninol analogs and methods of using the same to treat disorders.

GLYT2 MODULATORS

α-, β-, and γ-amino acid derivatives of formula I are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain. Formula I

Novel glycine transporter type-2 reuptake inhibitors. Part 2: β- and γ-amino acid derivatives

Several β- and γ-amino acid derivatives were prepared as glycine transport inhibitors and their ability to block the uptake of [ 14C]-glycine in COS7 cells transfected with human glycine transporter-2 (hGlyT-2) were evaluated. A range of lipoph

A novel synthesis of 1,3-benzodiazepin-2-ones using intramolecular heck reaction

The formation of the skeleton of 1,3-benzodiazepin-2-one could be efficiently achieved by intramolecular Heck reaction. This methodology was well applicable to the preparation of optically pure 4-substituted 1,3-benzodiazepin-2-ones starting from easily available α-amino acids.