165803-63-4

Upstream product

• 25574-11-2 3-(4-bromophenyl)propanol 
• 124-63-0 methanesulfonyl chloride 
• 1643-30-7 3-(4-bromophenyl)propionic acid 

Downstream Products

• 1318792-80-1 3-(4-bromophenyl)-N-(3-methoxypropyl)propan-1-amine 
• 1318792-81-2 tert-butyl N-[3-(4-bromophenyl)propyl]-N-(3-methoxypropyl)carbamate 
• 1318792-82-3 tert-butyl-(3-methoxypropyl)-N-{3-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]propyl}carbamate 
• 1318792-84-5 tert-butyl N-[3-{4-[5-amino-6-(3-pyridylcarbamoyl)pyrazin-2-yl]phenyl}propyl]-N-(3-methoxypropyl)carbamate 
• 1318792-63-0 AZD₇₉₂₉ 
• 1318792-64-1 3-amino-6-(4-{3-[(3-methoxypropyl)amino]propyl}phenyl)-N-pyridin-3-ylpyrazine-2-carboxamide mono-besylate 
• 1318792-65-2 3-amino-6-(4-{3-[(3-methoxypropyl)amino]propyl}phenyl)-N-pyridin-3-ylpyrazine-2-carboxamide mono-tosylate 
• 1318792-68-5 3-amino-6-(4-{3-[(3-methoxypropyl)amino]propyl}phenyl)-N-pyridin-3-ylpyrazine-2-carboxamide mono-DL-mandelate 
• 1046816-66-3 6-(3-(4-bromophenyl)propoxy)-2-(methylsulfonyl)-1,2,3,4-tetrahydroisoquinoline 

Relevant academic research and scientific papers

Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity

UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC) is a zinc metalloenzyme that catalyzes the first committed step in the biosynthesis of Lipid A, an essential component of the cell envelope of Gram-negative bacteria. The most advanced, disclosed LpxC inhibitors showing antibacterial activity coordinate zinc through a hydroxamate moiety with concerns about binding to other metalloenzymes. Here, we describe the discovery, optimization, and efficacy of two series of compounds derived from fragments with differing modes of zinc chelation. A series was evolved from a fragment where a glycine moiety complexes zinc, which achieved low nanomolar potency in an enzyme functional assay but poor antibacterial activity on cell cultures. A second series was based on a fragment that chelated zinc through an imidazole moiety. Structure-guided design led to a 2-(1S-hydroxyethyl)-imidazole derivative exhibiting low nanomolar inhibition of LpxC and a minimum inhibitory concentration (MIC) of 4 μg/mL against Pseudomonas aeruginosa, which is little affected by the presence of albumin.

Copper-Catalyzed Cross-Coupling between Alkyl (Pseudo)halides and Bicyclopentyl Grignard Reagents

The development of a copper-catalyzed cross-coupling between primary and secondary (pseudo)halides and bicyclopentyl Grignard reagents is reported. Highly strained bicyclopentanes can be cross-coupled with a large panel of primary alkyl mesylates and secondary alkyl iodides. The catalytic system is simple and cheap, and the reaction is general and chemoselective.

BIARYL DERIVATIVE AS GPR120 AGONIST

The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.

PYRAZINE DERIVATIVES

The invention concerns pyrazine derivatives of the Formula (I) or pharmaceutically-acceptable salts thereof; wherein each of n, m and R has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of bone-related disorders or conditions