23814-14-4

Upstream product

• 75-44-5 phosgene 
• 619-05-6 3,4-diaminobenzoic acid 
• 20632-43-3 3-ureido-benzoic acid 
• 57-13-6 urea 

Downstream Products

• 870090-73-6 2-oxo-2,3-dihydro-1H-benzoimidazolyl-N-(3,4-dibenzyloxyphenyl)-5-carboxamide 
• 933710-78-2 2- chloro-1H-1,3-benzodiazole-5-carboxylic acid 
• 1401461-19-5 N-(1-(7-(3,4-dimethoxyphenylamino)thiazolo[5,4-d]pyrimidin-5-yl)pyrrolidin-3-yl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazole-5-carboxamide 
• 683242-75-3 methyl 2-chloro-1H-benzo[d]imidazole-5-carboxylate 
• 864514-50-1 5-[3-(1-benzyl-piperidin-4-yl)-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-1,3-diethyl-1,3-dihydro-benzoimidazol-2-one 
• 459180-99-5 1,3-diethyl-5-(2-pyridin-3-yl-5-m-tolyl-3H-imidazol-4-yl)-1,3-dihydro-benzoimidazol-2-one 
• 459217-07-3 2-(1,3-diethyl-2-oxo-2,3-dihydro-1H-benzoimidazol-5-yl)-4-pyridin-3-yl-1-m-tolyl-butane-1,4-dione 
• 680189-18-8 1,3-diethyl-5-[2-oxo-2-(3-trifluoromethyl-phenyl)-ethyl]-1,3-dihydro-benzoimidazol-2-one 

Relevant academic research and scientific papers

Structural development studies of pyrazoloketone-derived acetyl-CoA carboxylase inhibitors

Acetyl-CoA carboxylase (ACC) plays a key role in fatty acid homeostasis in humans, and inhibitors of ACC are expected to inhibit fatty acid biosynthesis and to activate fatty acid β-oxidation. Therefore, they are considered to be candidates for treatment of metabolic syndrome and related diseases. In this context, an upstream kinase of ACC, adenosine monophosphate-activated protein kinase (AMPK), has also recently emerged as a potential therapeutic target, because it phosphorylates and inactivates ACC. Here, we designed a fused molecule consisting of a pyrazoloketone-type ACC inhibitor and a recently discovered AMPK activator, aiming to develop a novel combined ACC inhibitor/AMPK activator to regulate fatty acid levels. The designed compound was prepared through a convergent synthetic route. This compound and its methyl ester analogue showed potent ACC2-inhibitory activity with IC50 values of 8.8 and 1.3 μM, respectively. Exomethylene derivatives, obtained from an unexpected side reaction during deprotection, also exhibited ACC2-inhibitory activity.

Benzimidazolone p38 inhibitors

The synthesis and in vitro p38α activity of a novel series of benzimidazolone inhibitors is described. The p38α SAR is consistent with a mode of binding wherein the benzimidazolone carbonyl serves as the H-bond acceptor to Met109 of p38α in a manner analogous to the pyridine nitrogen of prototypical pyridylimidazole p38 inhibitors. Potent p38α activity comparable to that of several previously reported p38 inhibitors is observed for this novel chemotype.