2015 Journal of enzyme inhibition and medicinal chemistry
* Design, synthesis and evaluation of 3,4-dihydroxybenzoic acid derivatives as antioxidants, bio-metal chelating agents and acetylcholinesterase inhibitors.
- Metal ions, especially copper, zinc and iron, play an important role in the neurodegeneration process because they can affect protein misfolding, leading to the formation of the amyloid deposits and oxidative stress leading to reactive oxygen species (ROS). Here we report the synthesis and evaluation as antioxidant and metal chelating agents of 3,4-dihydroxybenzoic acid derivatives. Synthesized compounds were tested by the 2,2-diphenyl-2-picrylhydrazyl (DPPH) method showing a radical scavenging ability (EC50=0.093-0.118 μM) higher than Trolox used as reference. Furthermore, these compounds were able to bind both iron and copper, especially the iron (III), by the formation of hexa-coordinated complexes. Synthesized compounds were tested to evaluate their ability to inhibit acetyl- and butyryl-cholinesterase; the obtained results have demonstrated that they are selective inhibitors of AChE (Ki=1.5-18.9 μM) and result weakly active versus butyrylcholinesterase (BChE).
=>1.酸っぱい, 2.辛辣な, 3.酸, 4.《俗語》麻薬, LSD
Overview of noun acid
The noun acid has 2 senses (first 1 from tagged texts)
1. (4) acid -- (any of various water-soluble compounds having a sour taste and capable of turning
litmus red and reacting with a base to form a salt)
2. acid, back breaker, battery-acid, dose, dot, Elvis, loony toons, Lucy in the sky with diamonds,
pane, superman, window pane, Zen -- (street name for lysergic acid diethylamide)
Overview of adj acid
The adj acid has 3 senses (first 1 from tagged texts)
1. (1) acerb, acerbic, acid, acrid, bitter, blistering, caustic, sulfurous, sulphurous, virulent,
vitriolic -- (harsh or corrosive in tone; "an acerbic tone piercing otherwise flowery prose"; "a
barrage of acid comments"; "her acrid remarks make her many enemies"; "bitter words"; "blistering
criticism"; "caustic jokes about political assassination, talk-show hosts and medical ethics"; "a
sulfurous denunciation"; "a vitriolic critique")
2. acidic, acid, acidulent, acidulous -- (being sour to the taste)
3. acid -- (having the characteristics of an acid; "an acid reaction")
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