903886-76-0

Upstream product

• 3034-53-5 2-bromo-1,3-thiazole 
• 831-82-3 4-Phenoxyphenol 

Downstream Products

• 904962-08-9 2-{1-methyl-3-[2-(4-phenoxyphenoxy)-1,3-thiazol-5-yl]prop-2-ynyl}-1H-isoindole-1,3(2H)-dione 
• 903886-81-7 N-{1-methyl-3-[2-(4-phenoxyphenoxy)-1,3-thiazol-5-yl]prop-2-ynyl}acetamide 
• 903886-91-9 1-methyl-3-[2-(4-phenoxyphenoxy)-1,3-thiazol-5-yl]prop-2-ynylamine 
• 935266-71-0 N-benzothiazol-2-yl-N-{1-methyl-3-[2-(4-phenoxy-phenoxy)-thiazol-5-yl]-prop-2-ynyl}-4-nitro-benzenesulfonamide 
• 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 
• 935266-73-2 N-(3-methyl-isoxazol-5-yl)-N-{1-methyl-3-[2-(4-phenoxy-phenoxy)-thiazol-5-yl]-prop-2-ynyl}-4-nitro-benzenesulfonamide 
• 904962-56-7 N-(5-Methyl-isoxazol-3-yl)-N-{1-methyl-3-[2-(4-phenoxy-phenoxy)-thiazol-5-yl]-prop-2-ynyl}-4-nitro-benzenesulfonamide 
• 935266-74-3 N-(1-ethyl-1H-pyrazol-3-yl)-N-{1-methyl-3-[2-(4-phenoxy-phenoxy)-thiazol-5-yl]-prop-2-ynyl}-4-nitro-benzenesulfonamide 
• 935266-72-1 N-(1H-imidazol-2-yl)-N-{1-methyl-3-[2-(4-phenoxy-phenoxy)-thiazol-5-yl]-prop-2-ynyl}-4-nitro-benzenesulfonamide 
• 904962-27-2 N-isoxazol-3-yl-N-{1-methyl-3-[2-(4-phenoxy-phenoxy)-thiazol-5-yl]-prop-2-ynyl}-4-nitro-benzenesulfonamide 
• 935266-70-9 N-{1-methyl-3-[2-(4-phenoxy-phenoxy)-thiazol-5-yl]-prop-2-ynyl}-4-nitro-N-thiazol-2-yl-benzenesulfonamide 
• 904962-37-4 5-[3-(tert-butyl-dimethyl-silanyloxy)-but-1-ynyl]-2-(4-phenoxy-phenoxy)-thiazole 
• 903886-90-8 4-[2-(4-phenoxyphenoxy)-1,3-thiazol-5-yl]but-3-yn-2-ol 
• 903886-77-1 5-iodo-2-(4-phenoxyphenoxy)thiazole 

Relevant academic research and scientific papers

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.

Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy) thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors

A structurally novel acetyl-CoA carboxylase (ACC) inhibitor is identified from high-throughput screening. A preliminary structure-activity relationship study led to the discovery of potent dual ACC1/ACC2 and ACC2 selective inhibitors against human recombinant ACC1 and ACC2. Selective ACC2 inhibitors exhibited IC50 1000-fold selectivity against ACC1. (S)-Enantiomer 9p exhibited high ACC2 activity and lowered muscle malonyl-CoA dose-dependently in acute rodent studies, whereas (R)-enantiomer 9o was weak and had no effect on the malonyl-CoA level.

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.