99281-93-3

Upstream product

• 25508-33-2 dimethyl <(methylsulfonyl)methyl>phosphonate 
• 72155-45-4 Boc-L-phenylalaninal 
• 24424-99-5 di-tert-butyl dicarbonate 
• 66605-57-0 (S)-N-tert-butoxycarbonyl-2-amino-3-phenylpropanol 
• 40137-11-9 diethyl methylsulfonylmethylphosphonate 
• 3182-95-4 L-Phenylalaninol 
• 51987-73-6 (S)-2-tert-butoxycarbonylamino-3-phenyl-propionic acid methyl ester 
• 149451-80-9 (2S,3S)-3-(t-butoxycarbonylamino)-4-phenylbutane-1,2-diol 
• 116949-67-8 (2S,3S)-2-azido-1-phenyl-butane-3,4-diol 
• 98760-08-8 (1-oxiranyl-2-phenylethyl)carbamic acid tert-butyl ester 
• 78571-81-0 (R,R)-3-(phenylmethyl)oxiranemethanol 
• 42238-15-3 (2E)-4-phenylbut-2-en-1-ol 
• 799560-25-1 (2S,3S)-3-(tert-butoxycarbonylamino)-4-phenyl-1-methylsulfonyl-2-butanol 
• 799560-06-8 (2S,3S)-3-(tert-butoxycarbonylamino)-4-phenyl-1-methylthio-2-butanol 

Relevant academic research and scientific papers

Vinyl Sulfone-Based Inhibitors of Nonstructural Protein 2 Block the Replication of Venezuelan Equine Encephalitis Virus

Emerging infectious diseases like those caused by arboviruses such as Venezuelan equine encephalitis virus (VEEV) pose a serious threat to public health systems. Development of medical countermeasures against emerging infectious diseases are of utmost importance. In this work, an acrylate and vinyl sulfone-based chemical series was investigated as promising starting scaffolds against VEEV and as inhibitors of the cysteine protease domain of VEEV's nonstructural protein 2 (nsP2). Primary screen and dose response studies were performed to evaluate the potency and cytotoxicity of the compounds. The results provide structural insights into a new class of potent nonpeptidic covalent inhibitors of nsP2 cysteine protease represented by compound 11 (VEEV TrD, EC50= 2.4 μM (HeLa), 1.6 μM (Vero E6)). These results may facilitate the evolution of the compounds into selective and broad-spectrum anti-alphaviral drug leads.

Enantiodivergent, catalytic asymmetric synthesis of γ-amino vinyl sulfones

A set of diversely substituted N-Boc-γ-amino vinyl sulfones has been prepared by a four-step procedure from readily available, highly enantiopure anti-N-Boc-3-amino-1,2-alkanediols. This new route, which does not depend on the accessibility of α-amino acids as starting materials, is noteworthy for its efficiency, for its generality, and for the fact that both enantiomers of a given γ-amino vinyl sulfone can be obtained with equal ease.

Carboxyl-Modified Amino Acids and Peptides as Protease Inhibitors

Several types of carbonyl-modified amino acids and peptides were prepared in forms having N-terminal modifications (carrier fragments) suitable for one of several representative protease enzymes, and their inhibitory action toward those enzymes were evalu