Anti-Sporothrix Activity of Novel Copper-Itraconazole Complexes.
ChemMedChem
; 19(15): e202400054, 2024 Aug 01.
Article
em En
| MEDLINE
| ID: mdl-38669597
ABSTRACT
A series of new metal complexes, [Cu(ITZ)2Cl2] â
5H2O (1), [Cu(NO3)2(ITZ)2] â
3H2O â
C4H10O (2) and [Cu(ITZ)2)(PPh3)2]NO3 â
5H2O (3) were synthesized by a reaction of itraconazole (ITZ) with the respective copper salts under reflux. The metal complexes were characterized by elemental analyses, molar conductivity, 1H and 13C{1H} nuclear magnetic resonance, UV-Vis, infrared and EPR spectroscopies. The antifungal activity of these metal complexes was evaluated against the main sporotrichosis agents Sporothrix brasiliensis, Sporothrix schenkii, and Sporothrix globosa. All three new compounds inhibited the growth of S. brasiliensis and S. schenckii at lower concentrations than the free azole, with complex 2 able to kill all species at 4â
µM and induce more pronounced alterations in fungal cells. Complexes 2 and 3 exhibited higher selectivity and no mutagenic effect at the concentration that inhibited fungal growth and affected fungal cells. The strategy of coordinating itraconazole (ITZ) to copper was successful, since the corresponding metal complexes were more effective than the parent drug. Particularly, the promising antifungal activity of the Cu-ITZ complexes makes them potential candidates for the development of an alternative drug to treat mycoses.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sporothrix
/
Testes de Sensibilidade Microbiana
/
Itraconazol
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Cobre
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Complexos de Coordenação
/
Antifúngicos
Idioma:
En
Revista:
ChemMedChem
Assunto da revista:
FARMACOLOGIA
/
QUIMICA
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Brasil