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Efficient Synthesis and Neuroprotective Effect of Substituted 1,3-Diphenyl-2-propen-1-ones.

  作者 Jung, Jae-Chul;Jang, Soyong;Lee, Yongnam;Min, Dongguk;Lim, Eunyoung;Jung, Heyin;Oh, Miyeon;Oh, Seikwan;Jung, Mankil;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-13;  页码  4054-4058  
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[摘要]1, 22 An efficient synthesis involving a key aldol reaction and biol. properties of a series of 1,3-diphenyl-2-propen-1-ones is described. The in vitro activity for 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging of I and II (R1 = R2 = R3 = F) was 2 times higher than that for resveratrol. Compds. I (R1 = R2 = R3 = H; R1 = R2 = R3 = F) were the strongest in suppression of in vitro nitric oxide (NO) generation and antiexcitotoxicity. Mol. modeling proposes an electron-donating group at the para position of acetophenones that leads to a dramatic increase in the suppression of NO prodn.

 
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