21855-66-3

Upstream product

• 51513-97-4 N-[(phenylmethoxy)carbonyl]-β-alanine chloride 
• 110503-79-2 tert-butyl 2-(3-(((benzyloxy)carbonyl)amino)propanoyl)hydrazine-1-carboxylate 
• 501-53-1 benzyl chloroformate 
• 2304-94-1 3-(benzyloxycarbonylamino)propanoic acid 
• 54755-77-0 N-benzyloxycarbonyl-3-aminopropionic acid methyl ester 

Downstream Products

• 93767-92-1 bis(N-benzyloxycarbonyl-β-alanyl)diaza-18-crown-6 
• 1374459-02-5 3,7-anhydro-2-deoxy-4,5,6,8-tetra-O-acetyl-D-glycero-L-gulo-octose [(benzyloxycarbonyl)-(β)-Ala-oxycarbonyl]hydrazone 
• 21612-28-2 N^α-(N-benzyloxycarbonyl-β-alanyl)-histidine 
• 584-85-0 L-anserine 

Relevant academic research and scientific papers

Interest of new alkylsulfonylhydrazide-type compound in the treatment of alcohol use disorders

Rationale: Recent preclinical research suggested that histone deacetylase inhibitors (HDACIs) and specifically class I HDAC selective inhibitors might be useful to treat alcohol use disorders (AUDs). Objective: The objective of this study was to find a new inhibitor of the HDAC-1 isoenzyme and to test its efficacy in an animal model of AUDs. Methods: In the present study, we prepared new derivatives bearing sulfonylhydrazide-type zinc-binding group (ZBG) and evaluated these compounds in vitro on HDAC-1 isoenzyme. The most promising compound was tested on ethanol operant self-administration and relapse in rats. Results: We showed that the alkylsulfonylhydrazide-type compound (ASH) reduced by more than 55% the total amount of ethanol consumed after one intracerebroventricular microinjection, while no effect was observed on motivation of the animals to consume ethanol. In addition, one ASH injection in the central amygdala reduced relapse. Conclusions: Our study demonstrated that a new compound designed to target HDAC-1 is effective in reducing ethanol intake and relapse in rats and further confirm the interest of pursuing research to study the exact mechanism by which such inhibitor may be useful to treat AUDs.

COMPOUNDS, COMPOSITIONS, AND METHODS FOR INCREASING CFTR ACTIVITY

The invention encompasses compounds such as compounds having the Formula (I) or (II), compositions thereof, and methods of modulating CFTR activity. The invention also encompasses methods of treating a condition associated with CFTR activity or condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound.

Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 3CL Protease

Human noroviruses are the primary causative agents of acute gastroenteritis and a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the treatment or prophylaxis of norovirus infections. Norovirus 3CL protease plays a vital role in viral replication by generating structural and nonstructural proteins via the cleavage of the viral polyprotein. Thus, molecules that inhibit the viral protease may have potential therapeutic value. We describe herein the structure-based design, synthesis, and in vitro and cell-based evaluation of the first class of oxadiazole-based, permeable macrocyclic inhibitors of norovirus 3CL protease.

Synthesis of new C-glycosyl aza-β3-amino acids building blocks

New C-glycosylated Nβ-protected aza-β3- amino acid building blocks have been prepared from C-glycosyl aldehydes of gluco and galacto configuration by reductive amination and subsequent N-alkylation. These moieties were elaborated to