Liao, Liping published the artcileSynthesis and biological evaluation of 1,2,4-triazole derivatives as potential neuroprotectant against ischemic brain injury, Recommanded Product: 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is European Journal of Medicinal Chemistry (2020), 112114pp., database is CAplus and MEDLINE.
A series of 1,2,4-triazole derivatives I (R1 = H, OH; R2 = H, F, CF3, etc.; R3 = H, Me, F, CF3 ) was synthesized to investigate their neuroprotective effects and mechanisms of action. Some compounds noticeably protected PC12 cells from the cytotoxicity of H2O2 or sodium nitroprusside (SNP). Compound I (R1 = OH; R2 = OMe; R3 = H) was the most effective derivative Compound I (R1 = OH; R2 = OMe; R3 = H) chelated Fe (II) iron, scavenged reactive oxygen species (ROS), and restored the mitochondrial membrane potential (MMP). Moreover, it enhanced the activity of the antioxidant defense system by increasing the serum level of superoxide dismutase (SOD) and promoting the nuclear translocation of nuclear factor erythroid 2-related factor 2 (Nrf2). Compound I (R1 = OH; R2 = OMe; R3 = H) caused certain improvements in behavior, the cerebral infarction area, and serum levels of biochem. indicators (TNF-α, IL-1β, SOD and MDA) in a rat MCAO model. The LD (LD50) of compound I (R1 = OH; R2 = OMe; R3 = H) in mice receiving i.p. injections was greater than 400 mg/kg. Meanwhile, pharmacokinetic experiments revealed high bioavailability of this compound after both oral and i.v. administration (F = 60.76%, CL = 0.014 mg/kg/h) and a longer half-life (4.26 and 5.11 h after oral and i.v. administration, resp.). Based on these findings, compound I (R1 = OH; R2 = OMe; R3 = H) may be a promising neuroprotectant for the treatment of ischemic stroke.
European Journal of Medicinal Chemistry published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, Recommanded Product: 2-Hydroxy-4-(trifluoromethyl)benzoic acid.
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