| Author | Fonseca-Berzal, Cristina | |
| Author | Ibáñez-Escribano, Alexandra | |
| Author | Vela, Nerea | |
| Author | Cumella, José | |
| Author | Nogal-Ruiz, Juan José | |
| Author | Escario, José Antonio | |
| Author | Silva, Patrícia Bernardino da | |
| Author | Batista, Marcos Meuser | |
| Author | Soeiro, Maria de Nazaré C. | |
| Author | Sifontes-Rodríguez, Sergio | |
| Author | Meneses-Marcel, Alfredo | |
| Author | Gómez-Barrio, Alicia | |
| Author | Arán, Vicente J. | |
| Access date | 2019-02-08T16:51:17Z | |
| Available date | 2019-02-08T16:51:17Z | |
| Document date | 2018 | |
| Citation | FONSECA-BERZAL, Cristina; et al. Antichagasic, Leishmanicidal, and Trichomonacidal Activity of 2-Benzyl-5-nitroindazole-Derived Amines. ChemMedChem, v.13, p.1246-1259, 2018. | pt_BR |
| ISSN | 1860-7179 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/31499 | |
| Language | eng | pt_BR |
| Publisher | Wiley | pt_BR |
| Rights | restricted access | |
| Subject in Portuguese | Antiprotozoal agents | pt_BR |
| Subject in Portuguese | Leishmaniose | pt_BR |
| Subject in Portuguese | Heterociclos de nitrogênio | pt_BR |
| Subject in Portuguese | Tricomoníase | pt_BR |
| Subject in Portuguese | Tripanossomíase | pt_BR |
| Title | Antichagasic, Leishmanicidal, and Trichomonacidal Activity of 2-Benzyl-5-nitroindazole-Derived Amines | pt_BR |
| Type | Article | |
| DOI | 10.1002/cmdc.201800084 | |
| Abstract | 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. | pt_BR |
| Affilliation | Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Microbiologia y Parasitologia. Madrid, Spain. | pt_BR |
| Affilliation | Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Microbiologia y Parasitologia. Madrid, Spain. | pt_BR |
| Affilliation | Instituto de Química Médica. Consejo Superior de Investigaciones Científicas. Madrid, Spain. | pt_BR |
| Affilliation | Instituto de Química Médica. Consejo Superior de Investigaciones Científicas. Madrid, Spain. | pt_BR |
| Affilliation | Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Microbiologia y Parasitologia. Madrid, Spain. | pt_BR |
| Affilliation | Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Microbiologia y Parasitologia. Madrid, Spain. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidad Central “Marta Abreu” de Las Villas. Centro de Bioactivos Químicos. Vila Clara, Cuba. | pt_BR |
| Affilliation | Universidad Central “Marta Abreu” de Las Villas. Centro de Bioactivos Químicos. Vila Clara, Cuba. | pt_BR |
| Affilliation | Universidad Complutense de Madrid. Facultad de Farmacia. Departamento de Microbiologia y Parasitologia. Madrid, Spain. | pt_BR |
| Affilliation | Instituto de Química Médica. Consejo Superior de Investigaciones Científicas. Madrid, Spain. | pt_BR |
| Subject | Antiprotozoal agents | pt_BR |
| Subject | Leishmaniasis | pt_BR |
| Subject | Nitrogen heterocycles | pt_BR |
| Subject | Trichomoniasis | pt_BR |
| Subject | Trypanosomiasis | pt_BR |
| Embargo date | 2030-01-01 | |
