Department of Chemistry, University of Paderborn, Paderborn, Germany.
J Med Chem. 2011 Jul 14;54(13):4913-7. doi: 10.1021/jm200302d. Epub 2011 Jun 8.
New phenazines were synthesized by oxygenation of 1- and 2-naphthol with transition metal peroxo complexes and in situ reaction with 1,2-diamines. The title compounds were evaluated for in vitro antimalarial activity against Plasmodium falciparum and chloroquine-resistant strains. Phenazines 12, 27, and 28 were most prominent in growth inhibition. In vivo protection against cerebral malaria was observed with the phenazines 11, 12, 20, and 27, whereas partial protection was provided by 19.
新的吩嗪类化合物是通过过渡金属过氧配合物氧化 1- 和 2-萘酚，以及与 1,2-二胺的原位反应合成的。对这些标题化合物进行了体外抗疟活性评价，针对恶性疟原虫和氯喹抗性株。吩嗪 12、27 和 28 在生长抑制方面最为显著。吩嗪 11、12、20 和 27 对脑型疟疾具有体内保护作用，而 19 则提供了部分保护。
