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- W4284977299 abstract "In the current research, methaqualone derivatives were synthesized and assessed for their anti-convulsant activity. Among them, compounds 3, 4, 6, 7 and 11 exhibited significant anti-convulsant activities with ED50 values of 132.23 mg/kg, 120.34 mg/kg, 100.78 mg/kg, 145.89 mg/kg, and 148.46 mg/kg, respectively. The toxicity profiling (TD50) of these compounds (3, 4, 6, 7 and 11) demonstrated that these drugs caused only a minor neurological impairment. The PI scores of these compounds (3, 4, 6, 7 and 11) were higher than the reference drug (methaqualone PI: 1.99). The acetylcholinesterase enzyme level is significantly reduced in these compounds, indicating the enhancement of cognition activity. Pharmacophoric modelling and molecular docking studies against the human GABA-A receptor are in close agreement with each other. Molecular dynamic simulation of compound 6 indicates that it remains stable with the human GABA-A receptor for a 100 ns time span." @default.
- W4284977299 created "2022-07-10" @default.
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- W4284977299 date "2022-07-01" @default.
- W4284977299 modified "2023-10-14" @default.
- W4284977299 title "Time loops may be easier to achieve than we thought" @default.
- W4284977299 doi "https://doi.org/10.1016/s0262-4079(22)01193-9" @default.
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