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首页> 外文期刊>Journal of Medicinal Chemistry >In search of novel agents for therapy of tropical diseases and human immunodeficiency virus
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In search of novel agents for therapy of tropical diseases and human immunodeficiency virus

机译：寻找治疗热带病和人类免疫缺陷病毒的新型药物

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Malaria, sleeping sickness, Chagas' disease, Aleppo boil, and AIDS are among the tropical diseases causing millions of infections and cases of deaths per year because only inefficient chemotherapy is available. Since the targeting of the enzymes of the polyamine pathway may provide novel therapy options, we aimed to inhibit the deoxyhypusine hydroxylase, which is an important step in the biosynthesis of the eukaryotic initiation factor 5A. In order to identify new lead compounds, piperidines were produced and biologically evaluated. The 3,5-diethyl piperidone-3,5-dicarboxylates 11 and 13 substituted with 4-nitrophenyl rings in the 2 and 6 positions were found to be active against Trypanosoma brucei brucei and Plasmodium falciparum combined with low cytotoxicity against macrophages. The corresponding monocarboxylates are only highly active against the T. brucei brucei. The piperidine oximether 53 demonstrated the highest plasmodicidal activity. Moreover, compounds 11 and 53 were also able to inhibit replication of HIV-1.
机译：疟疾，昏睡病，恰加斯病，阿勒颇水煮和艾滋病是热带疾病，每年仅因无效的化学疗法而导致数百万的感染和死亡病例。由于靶向多胺途径的酶可能提供新颖的治疗选择，因此我们旨在抑制脱氧羟丝氨酸羟化酶，这是真核生物起始因子5A生物合成中的重要步骤。为了鉴定新的先导化合物，生产了哌啶并进行了生物学评估。发现在2和6位被4-硝基苯基环取代的3,5-二乙基哌啶酮-3,5-二羧酸酯11和13对布鲁氏锥虫和恶性疟原虫具有活性，并且对巨噬细胞具有低细胞毒性。相应的单羧酸盐仅对布鲁氏布鲁氏菌具有高活性。哌啶肟基醚53表现出最高的杀血浆活性。而且，化合物11和53也能够抑制HIV-1的复制。

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