ハロゲン化ピコリン酸誘導体／亜鉛（ＩＩ）錯体のインスリン様作用

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  • Insulinomimetic activity of zinc (II) complexes with halogenated picolinic acids.
  • ハロゲンカ ピコリンサン ユウドウタイ アエン 2 サクタイ ノ インスリン ヨウ サヨウ

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We prepared six new zinc(II) complexes of halogenated picolinic acids with a Zn(N2O2) coordination mode and evaluated for their insulinomimetic activities by in vitro study. By introducing an electron withdrawing halogen groups into the picolinic acid, we prepared bis(4- or 6-chloro picolinato), bis(4-, 5- or 6-iodo picolinato), and bis(6-bromo picolinato)/zinc(II) complexes (Zn(4cpa)2, Zn(6cpa)2, Zn(4ipa)2, Zn(5ipa)2, Zn(6ipa)2, and Zn(6bpa)2, respectively). By in vitro evaluation of the inhibition of free fatty acid (FFA) release from isolated rat adipocytes in the presence of epinephrine, the insulinomimetic activities of Zn(4cpa)2, Zn(6cpa)2, Zn(4ipa)2, Zn(6ipa)2, and Zn(6bpa)2 (IC50 = 0.64, 0.60, 0.77, 0.85, and 0.50 mM, respectvely) were found to be higher than that of bis(picolinato)/zinc(II) complex (Zn(pic)2) (IC50 = 1.00 mM) in terms of IC50 value, the 50% inhibition concentrations for the FFA release from rat adipocytes.

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