A new series of compounds （E）-1-（4-（bis-arylmethyl）piperazin-l-yl）-3-arylprop-2-en-1-one （1a-r）, have been synthesized and their structures were confirmed by ESI-MS and 1H NMR. The preliminary pharmacological ...A new series of compounds （E）-1-（4-（bis-arylmethyl）piperazin-l-yl）-3-arylprop-2-en-1-one （1a-r）, have been synthesized and their structures were confirmed by ESI-MS and 1H NMR. The preliminary pharmacological screening showed that some of these compounds had similar neuroprotective effects with Edaravone.展开更多
The crystal structure of the new cinnamide derivative（E）-1-（4-（4-chlorobenzyl）piperazin-1-yl）-3-（benzo[d][1,3]dioxol-5-yl）prop-2-en-1-one（C（21）H（21）ClN2O3, Mr = 384.85） was determined by single-crystal X...The crystal structure of the new cinnamide derivative（E）-1-（4-（4-chlorobenzyl）piperazin-1-yl）-3-（benzo[d][1,3]dioxol-5-yl）prop-2-en-1-one（C（21）H（21）ClN2O3, Mr = 384.85） was determined by single-crystal X-ray diffraction method. Compound 5 crystallizes in the monoclinic system, space group P21/c with a = 11.762（2）, b = 15.279（3）, c = 11.865（2） , β = 116.57（3）°, V = 1907.1（7） 3, Z = 4, Dc = 1.340 g/cm3, F（000） = 808, μ = 0.224 mm-1, Mo Kα radiation（λ = 0.71073 ）, the final R = 0.0565 and w R = 0.1479 for 2318 observed reflections with I 〉 2σ（I）. Intramolecular C（9）–H（9A）···O（1） interactions as well as intermolecular C（16）–H（16A）···O（1） hydrogen bonds help to stabilize the crystal structure. The bioassay results indicated that the title compound displayed promising neuroprotection in vitro and in vivo, and suppressed apoptosis of glutamate-induced PC12 cells.展开更多
A new cinnamide derivative,（E）-1-（4-（bis（4-methoxyphenyl）methyl）piperazin-1-yl）-3-（4-acetoxy-3-methoxyphenyl）prop-2-en-1-one（C31H34N2O6,Mr = 530.60）,has been synthesized by the condensation of 1-（bis（4-m...A new cinnamide derivative,（E）-1-（4-（bis（4-methoxyphenyl）methyl）piperazin-1-yl）-3-（4-acetoxy-3-methoxyphenyl）prop-2-en-1-one（C31H34N2O6,Mr = 530.60）,has been synthesized by the condensation of 1-（bis（4-methoxyphenyl）methyl）piperazine and（E）-3-（4-acetoxy-3-methoxyphenyl）acrylic acid.The compound was characterized by 1H NMR,13 C NMR,H RMS and single-crystal X-ray diffraction.The crystal belongs to the orthorhombic system,space group P212121 with a = 24.946（5）,b = 7.6380（15）,c = 14.555（3） A,V = 2773.3（10） A^3,Z = 4,Dc = 1.271 g/cm^3,F（000） = 1128,μ = 0.088 mm-1,Mo Kα radiation（λ = 0.71073 A）,the final R = 0.0641 and w R = 0.1170.A total of 3009 unique reflections were collected,of which 1760 with I 〉 2σ（I） were observed.Intramolecular C（17）–H（17B）···O（3） and C（22）–H（22A）···O（3） interactions as well as intermolecular C（27）–H（27A）···O（3） hydrogen bonds help to stabilize the crystal structure.The title compound was evaluated for the anti-ischemic activity in vitro and in vivo.The bioassay results indicated that the title compound displayed efficient activities against glutamine-induced neurotoxicity in PC12 cells and significantly prolonged the survival time of mice subjected to acute cerebral ischemia.展开更多
基金the Natural Science Foundation of Education Department of Jiangsu Province(No.05KJB350084).
文摘A new series of compounds （E）-1-（4-（bis-arylmethyl）piperazin-l-yl）-3-arylprop-2-en-1-one （1a-r）, have been synthesized and their structures were confirmed by ESI-MS and 1H NMR. The preliminary pharmacological screening showed that some of these compounds had similar neuroprotective effects with Edaravone.
基金Supported by the National Natural Science Foundation of China(No.81371451)the Natural Science Foundation of Jiangsu Province(No.BK20131390)
文摘The crystal structure of the new cinnamide derivative（E）-1-（4-（4-chlorobenzyl）piperazin-1-yl）-3-（benzo[d][1,3]dioxol-5-yl）prop-2-en-1-one（C（21）H（21）ClN2O3, Mr = 384.85） was determined by single-crystal X-ray diffraction method. Compound 5 crystallizes in the monoclinic system, space group P21/c with a = 11.762（2）, b = 15.279（3）, c = 11.865（2） , β = 116.57（3）°, V = 1907.1（7） 3, Z = 4, Dc = 1.340 g/cm3, F（000） = 808, μ = 0.224 mm-1, Mo Kα radiation（λ = 0.71073 ）, the final R = 0.0565 and w R = 0.1479 for 2318 observed reflections with I 〉 2σ（I）. Intramolecular C（9）–H（9A）···O（1） interactions as well as intermolecular C（16）–H（16A）···O（1） hydrogen bonds help to stabilize the crystal structure. The bioassay results indicated that the title compound displayed promising neuroprotection in vitro and in vivo, and suppressed apoptosis of glutamate-induced PC12 cells.
基金Supported by the National Natural Science Foundation of China(No.81371451)the Natural Science Foundation of Jiangsu Province(No.BK20131390)
文摘A new cinnamide derivative,（E）-1-（4-（bis（4-methoxyphenyl）methyl）piperazin-1-yl）-3-（4-acetoxy-3-methoxyphenyl）prop-2-en-1-one（C31H34N2O6,Mr = 530.60）,has been synthesized by the condensation of 1-（bis（4-methoxyphenyl）methyl）piperazine and（E）-3-（4-acetoxy-3-methoxyphenyl）acrylic acid.The compound was characterized by 1H NMR,13 C NMR,H RMS and single-crystal X-ray diffraction.The crystal belongs to the orthorhombic system,space group P212121 with a = 24.946（5）,b = 7.6380（15）,c = 14.555（3） A,V = 2773.3（10） A^3,Z = 4,Dc = 1.271 g/cm^3,F（000） = 1128,μ = 0.088 mm-1,Mo Kα radiation（λ = 0.71073 A）,the final R = 0.0641 and w R = 0.1170.A total of 3009 unique reflections were collected,of which 1760 with I 〉 2σ（I） were observed.Intramolecular C（17）–H（17B）···O（3） and C（22）–H（22A）···O（3） interactions as well as intermolecular C（27）–H（27A）···O（3） hydrogen bonds help to stabilize the crystal structure.The title compound was evaluated for the anti-ischemic activity in vitro and in vivo.The bioassay results indicated that the title compound displayed efficient activities against glutamine-induced neurotoxicity in PC12 cells and significantly prolonged the survival time of mice subjected to acute cerebral ischemia.
