Publicação
Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives
| Resumo: | In this work, 13 thiosemicarbazones (1a - m) and 16 thiazoles (2a - p) were obtained, which were properly characterized by spectroscopic and spectrometric techniques. The pharmacokinetic properties obtained in silico revealed that the derivatives are in accordance with the parameters established by lipinski and veber, showing that such compounds have good bioavailability or permeability when administered orally. In assays of antioxidant activity, thiosemicarbazones showed moderate to high antioxidant potential when compared to thiazoles. In addition, they were able to interact with albumin and DNA. Screening assays to assess the toxicity of compounds to mammalian cells revealed that thiosemicarbazones were less toxic when compared to thiazoles. In relation to in vitro antiparasitic activity, thiosemicarbazones and thiazoles showed cytotoxic potential against the parasites Leishmania amazonensis and Trypanosoma cruzi. Among the compounds, 1b, 1j and 2l stood out, showing inhibition potential for the amastigote forms of the two parasites. As for the in vitro antimalarial activity, thiosemicarbazones did not inhibit Plasmodium falciparum growth. In contrast, thiazoles promoted growth inhibition. This study shows in a preliminary way that the synthesized compounds have antiparasitic potential in vitro. |
|---|---|
| Autores principais: | Santos, Natali de França Nibbering |
| Outros Autores: | Junior, Natanael da Silva Bezerra; de Oliveira, Jamerson Ferreira; Duarte, Denise Maria Figueiredo Araújo; Dos Santos Soares, José Cleberson; Clara Marques, Diego Santa; da Silva Santos, Aline Caroline; Nogueira, Fátima; Alves Pereira, Valéria Rêgo; Alves de Lima, Maria Carmo; da Cruz Filho, Iranildo José |
| Assunto: | citotoxity in animal cells Leishmania Plasmodium falciparum Thiazoles/pharmacology Thiosemicarbazones/pharmacology Trypanosoma cruzi RM Therapeutics. Pharmacology QR Microbiology RA0421 Public health. Hygiene. Preventive Medicine Parasitology Pharmacology, Toxicology and Pharmaceutics(all) SDG 3 - Good Health and Well-being SDG 9 - Industry, Innovation, and Infrastructure |
| Ano: | 2023 |
| País: | Portugal |
| Tipo de documento: | artigo |
| Tipo de acesso: | acesso aberto |
| Instituição associada: | Universidade Nova de Lisboa |
| Idioma: | inglês |
| Origem: | Repositório Institucional da UNL |
| Resumo: | In this work, 13 thiosemicarbazones (1a - m) and 16 thiazoles (2a - p) were obtained, which were properly characterized by spectroscopic and spectrometric techniques. The pharmacokinetic properties obtained in silico revealed that the derivatives are in accordance with the parameters established by lipinski and veber, showing that such compounds have good bioavailability or permeability when administered orally. In assays of antioxidant activity, thiosemicarbazones showed moderate to high antioxidant potential when compared to thiazoles. In addition, they were able to interact with albumin and DNA. Screening assays to assess the toxicity of compounds to mammalian cells revealed that thiosemicarbazones were less toxic when compared to thiazoles. In relation to in vitro antiparasitic activity, thiosemicarbazones and thiazoles showed cytotoxic potential against the parasites Leishmania amazonensis and Trypanosoma cruzi. Among the compounds, 1b, 1j and 2l stood out, showing inhibition potential for the amastigote forms of the two parasites. As for the in vitro antimalarial activity, thiosemicarbazones did not inhibit Plasmodium falciparum growth. In contrast, thiazoles promoted growth inhibition. This study shows in a preliminary way that the synthesized compounds have antiparasitic potential in vitro. |
|---|