184644-22-2

Upstream product

• 19947-75-2 5-amino-3,4-dimethylisoxazol 
• 98-74-8 4-Nitrobenzenesulfonyl chloride 
• 4468-47-7 2-methyl-3-oxo-butyronitrile 

Downstream Products

• 127-69-5 sulfisoxazole 
• 393127-69-0 F₃₀₉₉-0019 
• 1394293-71-0 C₁₈H₁₆Cl₂N₄O₄S 
• 401578-21-0 C₁₈H₁₇ClN₄O₄S 
• 1394293-72-1 C₁₈H₁₆ClFN₄O₄S 
• 1394293-73-2 C₁₈H₁₆F₂N₄O₄S 
• 1394293-74-3 C₁₈H₁₆F₂N₄O₄S 
• 1394293-75-4 C₁₉H₁₇F₃N₄O₄S 
• 1394293-76-5 C₂₀H₂₂N₄O₆S 
• 904962-43-2 N-(3,4-dimethyl-isoxazol-5-yl)-N-{1-methyl-3-[2-(4-phenoxy-phenoxy)-thiazol-5-yl]-prop-2-ynyl}-4-nitro-benzenesulfonamide 

Relevant academic research and scientific papers

Virtual screening leads to the discovery of novel non-nucleotide P2Y 1 receptor antagonists

The P2Y1 receptor (P2Y1R) is a G protein-coupled receptor naturally activated by extracellular ADP. Its stimulation is an essential requirement of ADP-induced platelet aggregation, thus making antagonists highly sought compounds for the development of antithrombotic agents. Here, through a virtual screening campaign based on a pharmacophoric representation of the common characteristics of known P2Y1R ligands and the putative shape and size of the receptor binding pocket, we have identified novel antagonist hits of μM affinity derived from a N,N′-bis-arylurea chemotype. Unlike the vast majority of known P2Y 1R antagonists, these drug-like compounds do not have a nucleotidic scaffold or highly negatively charged phosphate groups. Hence, our compounds may provide a direction for the development of receptor probes with altered physicochemical properties.

The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: Polar region modifications

The structure-activity relationship study focused on the polar region of the HTS hit A-80040 (1) producing several series of potent and selective ACC2 inhibitors. The SAR suggests a compact lipophilic pocket that does not tolerate polar and ionic groups.

Novel acetyl-CoA carboxylase (ACC) inhibitors and their use in diabetes, obesity and metabolic syndrome

The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.