1417159-40-0

Upstream product

• 869116-13-2 Cbz-L-propargylglycine-OH 
• 1417159-39-7 methyl (S)-2-((S)-2-(((benzyloxy)carbonyl)amino)pent-4-ynamido)-4-methylpentanoate 
• 7517-19-3 methyl (L)-leucinate hydrochloride 
• 1443654-61-2 1-((1-methoxy-4-methyl-1-oxopentan-2-yl)amino)-1-oxopent-4-yn-2-aminium chloride 
• 208709-89-1 methyl 2-(2-((tert-butoxycarbonyl)amino)pent-4-ynamido)-4-methylpentanoate 
• 2666-93-5 (S)-Leu-OMe 

Downstream Products

• 1417159-36-4 methyl (6S,9S,12S)-12-(((benzyloxy)carbonyl)amino)-9-isobutyl-8,11-dioxo-1,7,10,15,16-pentaazabicyclo[12.2.1]heptadeca-14⁽¹⁷⁾,15-diene-6-carboxylate 
• 1417159-37-5 benzyl ((6S,9S,12S)-6-(hydroxymethyl)-9-isobutyl-8,11-dioxo-1,7,10,15,16-pentaazabicyclo[12.2.1]heptadeca-14⁽¹⁷⁾,15-dien-12-yl)carbamate 
• 1417159-38-6 benzyl ((6S,9S,12S)-6-formyl-9-isobutyl-8,11-dioxo-1,7,10,15,16-pentaazabicyclo[12.2.1]heptadeca-14⁽¹⁷⁾,15-dien-12-yl)carbamate 
• 1417159-41-1 methyl (5S,8S,11S)-11-(4-azidobutyl)-8-isobutyl-3,6,9-trioxo-1-phenyl-5-(prop-2-yn-1-yl)-2-oxa-4,7,10-triazadodecan-12-oate 
• 1443654-64-5 methyl 11-(3-((3-azidopropyl)amino)-3-oxopropyl)-8-isobutyl-3,6,9-trioxo-1-phenyl-5-(prop-2-yn-1-yl)-2-oxa-4,7,10-triazadodecan-12-oate 

Relevant academic research and scientific papers

Structure-based design and synthesis of triazole-based macrocyclic inhibitors of norovirus protease: Structural, biochemical, spectroscopic, and antiviral studies

Outbreaks of acute gastroenteritis caused by noroviruses constitute a public health concern worldwide. To date, there are no approved drugs or vaccines for the management and prophylaxis of norovirus infections. A potentially effective strategy for the development of norovirus therapeutics entails the discovery of inhibitors of norovirus 3CL protease, an enzyme essential for noroviral replication. We describe herein the structure-based design of the first class of permeable, triazole-based macrocyclic inhibitors of norovirus 3C-like protease, as well as pertinent X-ray crystallographic, biochemical, spectroscopic, and antiviral studies.

Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus

The design, synthesis, and in vitro evaluation of the first macrocyclic inhibitor of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus are reported. The in vitro inhibitory activity (50% effective concentration) of the macrocyclic inhibitor toward enterovirus 3C protease (CVB3 Nancy strain), and coronavirus (SARS-CoV) and norovirus 3C-like proteases, was determined to be 1.8, 15.5 and 5.1 μM, respectively.

MACROCYCLIC AND PEPTIDOMIMETIC COMPOUNDS AS BROAD-SPECTRUM ANTIVIRALS AGAINST 3C OR 3C-LIKE PROTEASES OF PICORNAVIRUSES, CALICIVIRUSES AND CORONAVIRUSES

Antiviral protease inhibitors, including macrocylic transition state inhibitors and peptidomimetics are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, sapoviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus.

New cylindrical peptide assemblies defined by extended parallel β-sheets

A new approach to non-covalent peptide-based nanotubular or rod-like structures is presented, whereby the monomeric units are preorganised into a β-strand geometry that templates the formation of an extended and unusual parallel β-sheet rod-like structure. The conformational constraint is introduced by Huisgen cycloaddition to give a triazole-based macrocycle, with the resulting self-assembled structures stabilized by a well-defined series of intermolecular hydrogen bonds. The Royal Society of Chemistry 2013.