| Revue: | Brazilian Journal of Pharmaceutical Sciences |
| Base de datos: | PERIÓDICA |
| Número de sistema: | 000451503 |
| ISSN: | 1984-8250 |
| Autores: | Pereira, Guilherme Rocha1 Ferreira, Andreza Cristina Gomes1 Neves, Pedro Henrique de Almeida Simões1 Gomes, Erick Bruman Souza1 Nascimento, Maria Fernanda Alves do2 Sousa, Jordano Augusto Carvalho2 Santos, Juliana de Oliveira3 Brandão, Geraldo Célio2 Oliveira, Alaíde Braga de3 |
| Instituciones: | 1Pontificia Universidade Catolica de Minas Gerais, Instituto de Ciencias Exatas e Informatica, Belo Horizonte, Minas Gerais. Brasil 2Universidade Federal de Ouro Preto, Escola de Farmacia, Ouro Preto, Minas Gerais. Brasil 3Universidade Federal de Minas Gerais, Faculdade de Farmacia, Belo Horizonte, Minas Gerais. Brasil |
| Año: | 2021 |
| Volumen: | 57 |
| País: | Brasil |
| Idioma: | Inglés |
| Tipo de documento: | Artículo |
| Enfoque: | Experimental, aplicado |
| Resumen en inglés | Malaria is nowadays one of the most serious health concerns in a global scale and, although there is an evident increase in research studies in this area, pointed by the vast number of hits and leads, it still appears as a recurrent topic every year due to the drug resistance shown by the parasite exposing the urgent need to develop new antimalarial medications. In this work, 38 molecules were synthesized via copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC) or “click” chemistry, following different routes to produce 2 different organic azides, obtained from a 4,7 dicholoquinoline, reacted with 19 different commercially available terminal alkynes. All those new compounds were evaluated for their in vitro activity against the chloroquine resistant malaria parasite Plasmodium falciparum (W2). The cytotoxicity evaluation was accomplished using Hep G2 cells and SI index was calculated for every molecule. Some of the quinoline derivatives have shown high antimalarial activity, with IC50 values in the range of 1.72-8.66 µM, low cytotoxicity, with CC50>1000 µM and selectivity index (SI) in the range of 20-100, with some compounds showing SI>800. Therefore, the quinolinotriazole hybrids could be considered a very important step on the development of new antimalarial drugs |
| Disciplinas: | Química |
| Palabras clave: | Microbiología, Química farmacéutica, Antimaláricos, Quinolinotrizoles, Síntesis química, Actividad biológica, Plasmodium falciparum |
| Keyword: | Microbiology, Medicinal chemistry, Antimalarial drugs, Quinolinotriazoles, Chemical synthesis, Biological activity, Plasmodium falciparum |
| Texte intégral: | Texto completo (Ver HTML) Texto completo (Ver PDF) |
