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Synthesis and Biological in vitro and in vivo Evaluation of 2‐(5‐Nitroindazol‐1‐yl)ethylamines and Related Compounds as Potential Therapeutic Alternatives for Chagas Disease
ChemMedChem ( IF 3.6 ) Pub Date : 2018-09-04 , DOI: 10.1002/cmdc.201800512 Rubén Martín-Escolano 1 , Benjamín Aguilera-Venegas 2 , Clotilde Marín 1 , Álvaro Martín-Montes 1 , Javier Martín-Escolano 1 , Encarnación Medina-Carmona 3 , Vicente J. Arán 4 , Manuel Sánchez-Moreno 1
ChemMedChem ( IF 3.6 ) Pub Date : 2018-09-04 , DOI: 10.1002/cmdc.201800512 Rubén Martín-Escolano 1 , Benjamín Aguilera-Venegas 2 , Clotilde Marín 1 , Álvaro Martín-Montes 1 , Javier Martín-Escolano 1 , Encarnación Medina-Carmona 3 , Vicente J. Arán 4 , Manuel Sánchez-Moreno 1
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Chagas disease, a neglected tropical disease caused by infection with the protozoan parasite Trypanosoma cruzi, is a potentially life‐threatening illness that affects 5–8 million people in Latin America, and more than 10 million people worldwide. It is characterized by an acute phase, which is partly resolved by the immune system, but then develops as a chronic disease without an effective treatment. There is an urgent need for new antiprotozoal agents, as the current standard therapeutic options based on benznidazole and nifurtimox are characterized by limited efficacy, toxicity, and frequent failures in treatment. In vitro and in vivo assays were used to identify some new low‐cost 5‐nitroindazoles as a potential antichagasic therapeutic alternative. Compound 16 (3‐benzyloxy‐5‐nitro‐1‐vinyl‐1H‐indazole) showed improved efficiency and lower toxicity than benznidazole in both in vitro and in vivo experiments, and its trypanocidal activity seems to be related to its effect at the mitochondrial level. Therefore, compound 16 is a promising candidate for the development of a new anti‐Chagas agent, and further preclinical evaluation should be considered.
中文翻译：
2-（5-硝基硝基吲哚-1-基）乙胺及相关化合物的合成及生物体内外评价，可作为查加斯病的潜在治疗选择
恰加斯病是一种被原生动物寄生虫克氏锥虫感染引起的被忽视的热带病，是一种潜在的威胁生命的疾病，影响了拉丁美洲5 800万人，全球超过1000万人。它的特征是急性期，部分由免疫系统解决，但随后发展成为一种慢性疾病，而没有有效的治疗方法。迫切需要新的抗原生动物剂，因为基于苯并咪唑和硝呋替莫斯的当前标准治疗选择的特征是疗效有限，毒性小且治疗失败频繁。体外和体内试验被用来确定一些新的低成本5-硝基吲唑作为潜在的抗chachagasic治疗替代品。化合物16（3-苄氧基-5-硝基-1-乙烯基-1- ħ -吲唑）显示出改善的效率和更低的毒性比在体外和体内实验苄硝唑在两者，并且其杀锥虫活性似乎在线粒体水平是相关的其效果。因此，化合物16是开发新型抗Chagas药物的有希望的候选者，应考虑进一步的临床前评估。
更新日期：2018-09-04
中文翻译：
2-（5-硝基硝基吲哚-1-基）乙胺及相关化合物的合成及生物体内外评价，可作为查加斯病的潜在治疗选择
恰加斯病是一种被原生动物寄生虫克氏锥虫感染引起的被忽视的热带病，是一种潜在的威胁生命的疾病，影响了拉丁美洲5 800万人，全球超过1000万人。它的特征是急性期，部分由免疫系统解决，但随后发展成为一种慢性疾病，而没有有效的治疗方法。迫切需要新的抗原生动物剂，因为基于苯并咪唑和硝呋替莫斯的当前标准治疗选择的特征是疗效有限，毒性小且治疗失败频繁。体外和体内试验被用来确定一些新的低成本5-硝基吲唑作为潜在的抗chachagasic治疗替代品。化合物16（3-苄氧基-5-硝基-1-乙烯基-1- ħ -吲唑）显示出改善的效率和更低的毒性比在体外和体内实验苄硝唑在两者，并且其杀锥虫活性似乎在线粒体水平是相关的其效果。因此，化合物16是开发新型抗Chagas药物的有希望的候选者，应考虑进一步的临床前评估。
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