Antifungal activity of Imidazolidin-4-ones of the antimalarial primaquine

• Author(s): Ferraz, Ricardo ; Fernandes, Rúben ; Vieira, Mónica ; Barros, P. ; Gomes, Paula ; Prudêncio, Cristina
• Date: 2005
• Persistent ID: http://hdl.handle.net/10400.22/2447
• Origin: Repositório Científico do Instituto Politécnico do Porto
• Document Type: Conference Object
• Language: English

Description

The 5-Isopropyl-3-[4-(6-methoxy-quinolin-8-ylamino)-pentyl]-2,2-dimethyl-imidazolidin-4-one (ValPQacet) was sinthesized through acylation of the anti-malarial primaquine with α-valine and subsequent reaction of the resulting -aminoamide with propanone (Sheme 1).Imidazolidin-4-ones of the anti malarial primaquine are being sinthesized to develop new variants in order to improve more effective treatments against malaria . Recently it has been observed that primaquine derivates could have effect in a new kind of yeast . To study the fungicidal activity against Candida albicans, Candida tropicalis, Issatchenkia orientalis, Sacharomyces cerevisae, the ValPQacet was put in the form of the hydrochloride salt. The minimal inhibitory concentration (MIC) could be determined for all yeast in the concentration range assayed. Also was determined MIC’s of primaquine hydrochloride salt for all yeast, and this shows that the parent drug is less active than our compound. Further studies are being performed to determine viability and cellular injury with this drugs.