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Synthesis and biological evaluation of H2S donor memantine derivatives / 中国药科大学学报
Journal of China Pharmaceutical University ; (6): 543-547, 2016.
Article in Chinese | WPRIM | ID: wpr-811858
ABSTRACT
@#H2S has a role of protecting neurons from ischemia-reperfusion injury and significantly reducing the cerebral infarction area, but high concentration of H2S can induce neurotoxicity. Memantine, a N-methyl-D-aspartic acid(NMDA)receptor antagonist, could reduce the neurotoxicity of H2S at high concentration. Nine novel structures(compounds I1-I9)were designed by coupling(4-hydroxy phenyl)-3H-1, 2-dithiole-3-thione(ADT-OH)with memantine through alkanes as linkers and synthesized by four-step reactions from ADT-OH. Their neuroprotection against damage induced by glutamate on HT-22 cells was evaluated by MTT method. The results indicated that these compounds markedly increased the survival rates of damaged HT-22 cells at the concentration of 1 μmol/L(P< 0. 01), which suggested that these compounds could preferably protect neurons against damage induced by glutamate.

Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Journal of China Pharmaceutical University Year: 2016 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Journal of China Pharmaceutical University Year: 2016 Type: Article