Synthesis and Biological Evaluation of Amphotericin B Formulations Based on Organic Salts and Ionic Liquids against Leishmania infantum

• Tipo: Artigo em Revista Científica Internacional
• Data: 2022

Autores

Ferraz, R (Autor) Outra; Santarem, N (Autor) Outra; Santos, AFM (Autor) Outra; Jacinto, ML (Autor) Outra; Anabela Cordeiro da Silva (Autor) FFUP; Prudencio, C (Autor) Outra; Noronha, JP (Autor) Outra; Branco, LC (Autor) Outra; Petrovski, Z (Autor) Outra

Revista

Título: Antibiotics

Vol. 11

Página Final: 1841

Editora: MDPI

Indexação

ISI Web of Knowledge - 2 Citações

Outras Informações

ID Authenticus: P-00X-TFC

DOI: 10.3390/antibiotics11121841

Abstract (EN): Nowadays, organic salts and ionic liquids (OSILs) containing active pharmaceutical ingredients (APIs) are being explored as drug delivery systems in modern therapies (OSILs-API). In that sense, this work is focused on the development of novel OSILs-API based on amphotericin B through an innovative procedure and the evaluation of the respective biological activity against Leishmania infantum. Several ammonium, methylimidazolium, pyridinium and phosphonium organic cations combined with amphotericin B as anion were synthesized in moderate to high yields and high purities by the water-reduced buffer neutralization method. All prepared compounds were characterized to confirm the desired chemical structure and the specific optical rotation ([alpha](D)(25)) was also determined. The biological assays performed on L. infantum promastigotes showed increased activity against this parasitic disease when compared with the starting chloride forms and amphotericin B alone, highlighting [P-6,P-6,P-6,P-14][AmB] as the most promising formulation. Possible synergism in the antiprotozoal activity was also evaluated for [P-6,P-6,P-6,P-14][AmB], since it was proven to be the compound with the highest toxicity. This work reported a simple synthetic method, which can be applied to prepare other organic salts based on molecules containing fragile chemical groups, demonstrating the potential of these OSILs-AmB as possible agents against leishmaniasis.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 12