110223-15-9Relevant articles and documents
Pyrazinyl ureas revisited: 1-(3-(Benzyloxy)pyrazin-2-yl)-3-(3,4-dichlorophenyl)urea, a new blocker of Aβ-induced mPTP opening for Alzheimer's disease
Elkamhawy, Ahmed,Park, Jung-eun,Hassan, Ahmed H.E.,Pae, Ae Nim,Lee, Jiyoun,Paik, Sora,Park, Beoung-Geon,Roh, Eun Joo
, p. 268 - 278 (2018)
Herein, we report synthesis and evaluation of new twenty-eight pyrazinyl ureas against β amyloid (Aβ)-induced opening of mitochondrial permeability transition pore (mPTP) using JC-1 assay which measures the change of mitochondrial membrane potential (ΔΨm). The neuroprotective effect of seventeen compounds against Aβ-induced mPTP opening was superior to that of the standard Cyclosporin A (CsA). Among them, 1-(3-(benzyloxy)pyrazin-2-yl)-3-(3,4-dichlorophenyl)urea (5) effectively maintained mitochondrial function and cell viabilities on ATP assay and MTT assay. Also, hERG channel assay presented safe cardiotoxicity profile for compound 5. In addition, using CDocker algorithm, a molecular docking model presented a plausible explanation for the elicited differences in efficiencies of the synthesized compounds to reduce the green to red fluorescence as indication of mPTP closure. Hence, this report presents compound 5 as the most promising pyrazinyl urea-based mPTP blocker up to date.
Urea analogs as neuroprotective agents
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Paragraph 0797; 0798, (2016/10/07)
In the brain the present invention refers to mPTP mitochondrial the selectively inhibit action of the improvement of the function of acting as an a neuro-protective agent central nervous system a using the zero therapeutic or prophylactic treatment of a disorder urea derivatives or a pharmaceutically acceptable salt, manufacturing method of these compounds, and methods of using these compounds is pharmaceutical composition contain as the active ingredient an relates.
IMIDAZO COMPOUNDS AND USES THEREOF
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Page/Page column 43-44, (2008/06/13)
N-substituted imidazopyrazinone compounds such as N-alkylated/aralkylated 7H-imidazo[1,2-a]pyrazin-8-one compounds and related analogs are disclosed. Pharmaceutical compositions and kits containing the N-substituted imidazopyrazinone compounds, as well as therapeutic uses thereof, including treatment of arrhythmia, are also disclosed.