Efficient Inhibition of Iron Superoxide Dismutase and of Trypanosoma cruzi Growth by Benzo[g]phthalazine Derivatives Functionalized with One or Two Imidazole Rings

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• 作者：Ana M. Sanz ; Fernando Gó ; mez-Contreras ; Pilar Navarro ; Manuel Sá ; nchez-Moreno ; Samira Boutaleb-Charki ; Jose Campuzano ; Mercedes Pardo ; Antonio Osuna ; Carmen Cano ; Marí ; a J. R. Yunta ; Lucrec
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：March 27, 2008
• 年：2008
• 卷：51
• 期：6
• 页码：1962 - 1966
• 全文大小：116K
• 年卷期：v.51,no.6(March 27, 2008)
• ISSN：1520-4804

文摘

The synthesis and trypanosomatic behavior of a new series of 1,4-bis(alkylamino)benzo[g]phthalazines 1−4 containing the biologically significant imidazole ring are reported. In vitro antiparasitic activity against Trypanosoma cruzi epimastigotes is remarkable, especially for compound 2, whereas toxicity against Vero cells is very low. Conversion of epimastigotes to metacyclic forms in the presence of the tested compounds causes significant decreases in the amastigote and trypomastigote numbers. Fe-SOD inhibition is noteworthy, whereas effect on human Cu/Zn-SOD is negligible.