Cheng, Hua; Yang, Lu; Liu, Hong-Fu; Zhang, Rui; Chen, Cheng; Wu, Yuan; Jiang, Wen published the artcile< N-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)picolinamide as a new inhibitor of mitochondrial complex III: Synthesis, biological evaluation and computational simulations>, Application In Synthesis of 81107-97-3, the main research area is chlorotrifluoromethylphenoxyphenylpicolinamide preparation mitochondria complex III inhibitor; Amide; Biological evaluation; Computational simulation; Diaryl ether; Inhibitor; Mitochondrial complex III.
Mitochondrial complex III is one of the most promising targets for a number of pharmaceuticals and fungicides. Due to the wide-spread use of complex III-inhibiting fungicides, a considerable increase of resistance occurred worldwide. Therefore, inhibitors with novel scaffolds and potent activity against complex III are still in great demand. A new series of amide compounds bearing the diaryl ether scaffold were designed and prepared, followed by the biol. evaluation. Gratifyingly, several compounds demonstrated potent activity against succinate-cytochrome c reductase (SCR, a mixture of mitochondrial complex II and complex III), with compound N-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)picolinamide possessing the best inhibitory activity (IC50 = 0.91 ± 0.09μmol/L). Addnl. studies verified that N-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)picolinamide was a new inhibitor of complex III. Moreover, computational simulations elucidated that N-(4-(2-chloro-4-(trifluoromethyl)phenoxy)phenyl)picolinamide should bind to the Qo site of complex III. The authors believe this work will be valuable for the preparation and discovery of more complex III inhibitors.
Bioorganic & Medicinal Chemistry Letters published new progress about 81107-97-3. 81107-97-3 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3O, Application In Synthesis of 81107-97-3.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary