Silva, Leticia B. published the artcile7-Amine-spiro[chromeno[4,3-b]quinoline-6,1′-cycloalkanes]: Synthesis and cholinesterase inhibitory activity of structurally modified tacrines, Formula: C7H6N2, the main research area is spirochromenoquinolinecycloalkan amine preparation cholinesterase inhibition SAR mol docking; Acetylcholinesterase (AChE); Alzheimer’s disease; Butyrylcholinesterase (BChE); Docking; Quinolone; Spirochromene; Tacrine.
Five new examples of 9,10-chloro(bromo)-7-amine-spiro[chromeno[4,3-b]quinoline-6,1′-cycloalkanes] I [R = H, Me; n = 0, 1,2; Z = 9-chloro, 10-chloro, 9-bromo, etc.] were synthesized at yields of 42-56%, using a sequential one-pot two-step cyclocondensation reaction of three different scaffolds of 2-aminobenzonitriles and the resp. spiro[chroman-2,1′-cycloalkan]-4-ones, and using AlCl3 as the catalyst in a solvent-free method. Subsequently, the five new spirochromeno-quinolines and nine quinolines I were subjected to AChE and BChE inhibitory activity evaluation. The mol. containing a spirocyclopentane derivative I had the highest AChE and BChE inhibitory activity (IC50 = 3.60 and 4.40μM, resp.), and in general, the non-halogenated compounds were better inhibitors of AChE and BChE than the halogenated mols. However, the inhibitory potency of compounds I synthesized was weaker than that of tacrine. By mol. docking simulations, it was found that the size of the spirocarbocyclic moieties I was inversely proportional to the inhibitory activity of the cholinesterases, probably because an increase in the size of the spirocyclic component sterically hindered the interaction of tacrine derivatives with the active site of tested cholinesterases. The findings obtained here was helped in the design and development of new anticholinesterase drugs.
Bioorganic Chemistry published new progress about Cholinesterase inhibitors. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Formula: C7H6N2.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts