Tu, Shun published the artcileN-(3-cyano-1H-indol-5-yl)isonicotinamide and N-(3-cyano-1H-indol-5-yl)-1H-benzo[d]imidazole-5-carboxamide derivatives: Novel amide-based xanthine oxidase inhibitors, Synthetic Route of 1453-82-3, the publication is Bioorganic Chemistry (2021), 105181, database is CAplus and MEDLINE.
Our previous work demonstrated that amide is an efficient linker to explore chem. space of xanthine oxidase (XO) inhibitors that are entirely different from febuxostat and topiroxostat. In this effort, with 3-cyano-1H-indol-5-yl as a key moiety, two series of amide-based XO inhibitors, N-(3-cyano-1H-indol-5-yl)isonicotinamides and N-(3-cyano-1H-indol-5-yl)-1H-benzo[d]imidazole-5-carboxamides, were designed and synthesized. The structure-activity relationship investigation identified N-(3-cyano-1-cyclopentyl-1H-indol-5-yl)-1H-benzo[d]imidazole-5-carboxamide (I, IC50 = 0.62μM) as the most promising compound, with 14.4-fold higher in vitro inhibitory potency than allopurinol (IC50 = 8.91μM). Mol. simulations provided reasonable interaction modes for the representative compounds Furthermore, in vivo activity evaluation demonstrated that compound I (oral dose of 12.8 mg/kg) has obviously hypouricemic effect on a potassium oxonate induced hyperuricemic rat model. Cytotoxicity assay and ADME prediction also supported that I is an excellent lead for further exploration of amide-based XO inhibitors.
Bioorganic Chemistry published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C17H28ClNO3, Synthetic Route of 1453-82-3.
Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics