Sanz Ana M, Gómez-Contreras Fernando, Navarro Pilar, Sánchez-Moreno Manuel, Boutaleb-Charki Samira, Campuzano Jose, Pardo Mercedes, Osuna Antonio, Cano Carmen, Yunta María J R, Campayo Lucrecia
Departamento de Química Orgánica I, Facultad de Química, Universidad Complutense, Madrid, Spain.
J Med Chem. 2008 Mar 27;51(6):1962-6. doi: 10.1021/jm701179m. Epub 2008 Feb 23.
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.
报道了一系列含有具有生物学意义的咪唑环的新型1,4-双(烷基氨基)苯并[g]酞嗪1-4的合成及其对锥虫的作用。体外对克氏锥虫前鞭毛体的抗寄生虫活性显著,尤其是化合物2,而对Vero细胞的毒性非常低。在受试化合物存在下,前鞭毛体向循环后期形式的转化导致无鞭毛体和锥鞭毛体数量显著减少。值得注意的是对铁超氧化物歧化酶(Fe-SOD)的抑制作用,而对人铜/锌超氧化物歧化酶(Cu/Zn-SOD)的影响可忽略不计。