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Antichagasic, Leishmanicidal, and Trichomonacidal Activity of 2‐Benzyl‐5‐nitroindazole‐Derived Amines
ChemMedChem ( IF 3.6 ) Pub Date : 2018-05-22 , DOI: 10.1002/cmdc.201800084 Cristina Fonseca-Berzal 1 , Alexandra Ibáñez-Escribano 1 , Nerea Vela 2 , José Cumella 2 , Juan José Nogal-Ruiz 1 , José Antonio Escario 1 , Patrícia Bernardino da Silva 3 , Marcos Meuser Batista 3 , Maria de Nazaré C. Soeiro 3 , Sergio Sifontes-Rodríguez 4 , Alfredo Meneses-Marcel 4 , Alicia Gómez-Barrio 1 , Vicente J. Arán 2
ChemMedChem ( IF 3.6 ) Pub Date : 2018-05-22 , DOI: 10.1002/cmdc.201800084 Cristina Fonseca-Berzal 1 , Alexandra Ibáñez-Escribano 1 , Nerea Vela 2 , José Cumella 2 , Juan José Nogal-Ruiz 1 , José Antonio Escario 1 , Patrícia Bernardino da Silva 3 , Marcos Meuser Batista 3 , Maria de Nazaré C. Soeiro 3 , Sergio Sifontes-Rodríguez 4 , Alfredo Meneses-Marcel 4 , Alicia Gómez-Barrio 1 , Vicente J. Arán 2
Affiliation
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Three different series of new 5‐nitroindazole derivatives—1‐(ω‐aminoalkyl)‐2‐benzylindazolin‐3‐ones (series A; ten compounds), 3‐(ω‐aminoalkoxy)‐2‐benzylindazoles (series B; four compounds) and 3‐alkylamino‐2‐benzylindazoles (series C; five compounds)—have been synthesized and evaluated against the protozoan parasites Trypanosoma cruzi, Leishmania amazonensis, and Trichomonas vaginalis: etiological agents of Chagas disease, cutaneous leishmaniasis, and trichomoniasis, respectively. Many indazoles of series A, B, and C were efficient against T. cruzi. Some compounds in series A, after successfully passing the preliminary screening for epimastigotes, exhibited activity values against amastigotes of several T. cruzi strains that were better than or similar to those shown by the reference drug benznidazole and displayed low nonspecific toxicity against mammalian cells. On the other hand, preliminary studies against promastigotes of L. amazonensis showed high leishmanicidal activity for some derivatives of series A and C. With regard to activity against T. vaginalis, some indazoles of series B and C were rather efficient against trophozoites of a metronidazole‐sensitive isolate and showed low nonspecific toxicities toward Vero cell cultures. Additionally, some of these compounds displayed similar activity against metronidazole‐sensitive and resistant isolates, showing the absence of cross‐resistance between these derivatives and the reference drug.
中文翻译：
2-苄基5-硝基吲哚衍生的胺类的抗chachagas，Leishmanicdal和Trichomonacidal活性
三种不同的新5-硝基吲唑衍生物-1-（ω-氨基烷基）-2-苄基吲唑啉-3-（A系列;十种化合物），3-（ω-氨基烷氧基）-2-苄基吲唑（B系列;四种化合物）和3-烷基氨基-2-苄基吲唑（C系列；五个化合物）—分别针对原生动物的寄生虫锥虫，利什曼原虫和亚马逊毛滴虫：Chagas病，皮肤利什曼病和滴虫病的病原体进行了评估。许多A，B和C系列的吲唑均能有效地抵抗克氏锥虫（T. cruzi）。串联的一些化合物甲，后成功通过初步筛选epimastigotes，对几种的无鞭毛体展示的活性值锥虫了比更好或类似的由参考药物苄硝唑示出的那些和显示针对哺乳动物细胞的低非特异性毒性菌株。另一方面，针对亚马逊L. amasonensis的前鞭毛体的初步研究显示，对于系列A和C的某些衍生物，其杀螨活性很高。关于抗阴道毛滴虫的活性，一些B和C系列的吲唑对甲硝唑敏感菌的滋养体相当有效，并且对Vero细胞培养物的非特异性毒性低。此外，这些化合物中的一些对甲硝唑敏感性和耐药性分离株表现出相似的活性，表明这些衍生物与参考药物之间没有交叉耐药性。
更新日期：2018-05-22
中文翻译：
2-苄基5-硝基吲哚衍生的胺类的抗chachagas，Leishmanicdal和Trichomonacidal活性
三种不同的新5-硝基吲唑衍生物-1-（ω-氨基烷基）-2-苄基吲唑啉-3-（A系列;十种化合物），3-（ω-氨基烷氧基）-2-苄基吲唑（B系列;四种化合物）和3-烷基氨基-2-苄基吲唑（C系列；五个化合物）—分别针对原生动物的寄生虫锥虫，利什曼原虫和亚马逊毛滴虫：Chagas病，皮肤利什曼病和滴虫病的病原体进行了评估。许多A，B和C系列的吲唑均能有效地抵抗克氏锥虫（T. cruzi）。串联的一些化合物甲，后成功通过初步筛选epimastigotes，对几种的无鞭毛体展示的活性值锥虫了比更好或类似的由参考药物苄硝唑示出的那些和显示针对哺乳动物细胞的低非特异性毒性菌株。另一方面，针对亚马逊L. amasonensis的前鞭毛体的初步研究显示，对于系列A和C的某些衍生物，其杀螨活性很高。关于抗阴道毛滴虫的活性，一些B和C系列的吲唑对甲硝唑敏感菌的滋养体相当有效，并且对Vero细胞培养物的非特异性毒性低。此外，这些化合物中的一些对甲硝唑敏感性和耐药性分离株表现出相似的活性，表明这些衍生物与参考药物之间没有交叉耐药性。
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