New Insulinomimetic Zinc(II) Complexes of Nicotinamide and its Derivatives: X-ray Structure and Biochemical Activity

Three Zn(II) complexes with nicotinamide(na), nicotinemethylamide(nma), and nicotineethylamide(nea) were found to have in vitro insulinomimetic activities. X-ray structure analysis of [Zn(nea)2(H2O)2(SO4)]n showed that each nitrogen atom of two nea molecules locates trans, and the two water molecule...

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Veröffentlicht in:Chemistry letters 2001, Vol.30 (11), p.1184-1185
Hauptverfasser: Ueda, Eriko, Yoshikawa, Yutaka, Kishimoto, Noriko, Tadokoro, Makoto, Yanagihara, Naohisa, Sakurai, Hiromu, Kojima, Yoshitane
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Sprache:eng
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Zusammenfassung:Three Zn(II) complexes with nicotinamide(na), nicotinemethylamide(nma), and nicotineethylamide(nea) were found to have in vitro insulinomimetic activities. X-ray structure analysis of [Zn(nea)2(H2O)2(SO4)]n showed that each nitrogen atom of two nea molecules locates trans, and the two water molecules and each oxygen atom of the two sulfates coordinate to a Zn(II) ion, forming an octahedral geometry of Zn(N2O4) unit in an inorganic polymer crystal. The Zn(II) complexes with na, nma, and nea exhibited higher insulinomimetic activities, respective IC50 values (50% inhibition concentration of the complex in the free fatty acids release from rat adipocytes) being 1.34, 1.12, and 0.96 mM, than that of ZnSO4 (IC50 = 1.52 mM).
ISSN:0366-7022
1348-0715
DOI:10.1246/cl.2001.1184