- A 2 - [2 - (3-methoxy-phenyl)-ethyl]-phenol synthesis method
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The invention discloses a synthetic method for 2-[2-(3-methoxyphenyl)ethyl]phenol. The method comprises: firstly synthesizing diethyl 3-methoxybenzylphosphonate and 2,2-dimethoxybenzaldehyde, then successively synthesizing 1-(2,2-dimethoxyphenyl)-2-(3-methoxyphenyl)ethylene, 1-(2-phenoxy)-2-(3-methoxyphenyl)ethylene, 1-(2-acetoxphenyl)-2-(3-methoxyphenyl)ethylene and 1-(2-acetoxphenyl)-2-(3-methoxyphenyl)ethane, and finally synthesizing the product 2-[2-(3-methoxyphenyl)ethyl]phenol. The prepared 2-[2-(3-methoxyphenyl)ethyl]phenol product is good in quality and high in yield.
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- SAR study on arylmethyloxyphenyl scaffold: Looking for a P-gp nanomolar affinity
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Starting from the previously developed P-gp ligands 1a and 1b (EC 50 = 0.25 μM and 0.65 μM, respectively), new arylmethyloxyphenyl derivatives have been synthesized as P-gp modulators in order to investigate: (i) the effect of small electron-do
- Nesi, Giulia,Colabufo, Nicola Antonio,Contino, Marialessandra,Perrone, Maria Grazia,Digiacomo, Maria,Perrone, Roberto,Lapucci, Annalina,Macchia, Marco,Rapposelli, Simona
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p. 558 - 566
(2014/04/03)
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- 1-PHENYLALCOXY-2-BETA-PHENYLETHYL DERIVATIVES AS P-GLYCOPROTEIN (P-GP) INHIBITORS USEFUL IN DRUG RESISTANCE EVENTS
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The invention relates to a new class of compounds, which are 1-phenylalcoxy-2-β-phenylethyl derivatives, as P-glycoprotein (P-GP) inhibitors. These compounds are useful in drug resistance events. They have been shown able to inhibit in a dose-dependent ma
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Page/Page column 10
(2009/04/24)
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- Arylmethyloxyphenyl derivatives: Small molecules displaying P-glycoprotein inhibition
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Some arylmethyloxyphenyl derivatives were prepared as simplified structures of analogous arylpiperazines with high affinity toward dopaminergic D 2 and serotonergic 5-HT1A receptors and inhibiting P-glycoprotein (P-gp). The compounds 5b and 8b displayed good P-gp inhibition activity measured as [3H]vinblastine transport inhibition in the Caco-2 cell monolayer and intracellular doxorubicin accumulation in MCF7/Adr cells by flow cytometry. Compounds 5b and 8b also inhibited, dose-dependently, ATP-ase activation induced by P-gp substrate vinblastine.
- Colabufo, Nicola Antonio,Berardi, Francesco,Perrone, Roberto,Rapposelli, Simona,Digiacomo, Maria,Balsamo, Aldo
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p. 6607 - 6613
(2007/10/03)
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- Syntheses and Platelet Aggregation Inhibitory and Antithrombotic Properties of ethyl>benzenes
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A series of ethyl>benzene derivatives were synthesized and evaluated for their ability to inhibit collagen-induced platelet aggregation in vitro and to protect experimantal thrombosis in mice.The results showed that the compounds were in vitro inhibitors of collagen-induced platelet aggregation.Most of them were also effective in the mouse antithrombotic assay.The compounds were found to be potent antagonists to S2 serotonergic receptor, and good correlation (r = 0.85) between their S2 serotonergic receptor antagonism and their potency as platelet antiaggregatory drugs was observed.Among the compounds studied, monophenoxy>methyl>ethyl>succinate hydrochloride (12b, MCI-9042) was selected for further pharmacological and toxicological evaluation.
- Kikumoto, Ryoji,Hara, Hiroto,Ninomiya, Kunihiro,Osakabe, Masanori,Sugano, Mamoru,et al.
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p. 1818 - 1823
(2007/10/02)
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