- Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents
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In this paper, we designed and synthesized a series of novel phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents. The best compound 10 had relatively high affinity for the GABAA receptor and low affinity for thirteen other off-target receptors. In three animal models (mice, rats, and rabbits), compound 10 exerted potent hypnotic effects (HD50 = 5.2 mg/kg in rabbits), comparable duration of the loss of righting reflex (LORR), and significant shorter recovery time (time to walk) than propanidid. Furthermore, compound 10 (TI = 18.1) showed higher safety profile than propanidid (TI = 14.7) in rabbits. Above results suggested that compound 10 may have predictable and rapid recovery profile in anesthesia.
- Chen, Yin,Huang, Ling,Li, Ziying,Qi, Zhaoyang,Zhang, Guisen,Zhang, Xiaohua,Zhu, Mo,Zhuang, Tao
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- Synthesis and evaluation of 4-hydroxyphenylacetic acid amides and 4-hydroxycinnamamides as antioxidants
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4-Hydroxyphenylacetic acid amides and 4-hydroxycinnamamides were synthesized and their antioxidant and neuroprotective activities were evaluated. Among the prepared compounds, 6f, 6g, 8b, and 9 exhibited potent inhibition of lipid peroxidation in rat brain homogenates, and marked DPPH radical scavenging activities. Furthermore, 6f, 6g, and 9 exhibited neuroprotective action against the oxidative damage induced by the exposure of primary cultured rat cortical cells to H2O2, xanthine/xanthine oxidase, or Fe2+/ascorbic acid. Based on these results, we found that 6f was the most potent antioxidant among the compounds tested.
- Jung, Young-Sik,Kang, Tae-Souk,Yoon, Joong-Ho,Joe, Bo-Young,Lim, Hee-Jong,Seong, Churl-Min,Park, Woo-Kyu,Kong, Jae-Yang,Cho, Jungsook,Park, No-Sang
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p. 2599 - 2602
(2007/10/03)
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- Synthesis of 3-alkoxy-4-hydroxyphenylacetic acids from methyl 3-alkoxybenzoates
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3-Alkoxy-4-hydroxyphenylacetic acids 4 were obtained from 3-alkoxyl-substituted methyl benzoates 1 by reductive alkylation, followed by allylic oxidation and hydrolysis.
- Jung,Kang,Lee,Seong,Ham,Park
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p. 455 - 462
(2007/10/03)
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