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Potent Synergy between Spirocyclic Pyrrolidinoindolinones and Fluconazole against Candida albicans.

ABSTRACT: A spiroindolinone, (1S,3R,3aR,6aS)-1-benzyl-6'-chloro-5-(4-fluorophenyl)-7'-methylspiro[1,2,3a,6a-tetrahydropyrrolo[3,4-c]pyrrole-3,3'-1H-indole]-2',4,6-trione, was previously reported to enhance the antifungal effect of fluconazole against Candida albicans. A diastereomer of this compound was synthesized, along with various analogues. Many of the compounds were shown to enhance the antifungal effect of fluconazole against C.?albicans, some with exquisite potency. One spirocyclic piperazine derivative, which we have named synazo-1, was found to enhance the effect of fluconazole with an EC50 value of 300?pM against a susceptible strain of C.?albicans and going as low as 2?nM against some resistant strains. Synazo-1 exhibits true synergy with fluconazole, with an FIC index below 0.5 in the strains tested. Synazo-1 exhibited low toxicity in mammalian cells relative to the concentrations required for antifungal synergy.

SUBMITTER: Premachandra ID 

PROVIDER: S-EPMC4682886 | biostudies-literature | 2015 Oct

REPOSITORIES: biostudies-literature

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Potent Synergy between Spirocyclic Pyrrolidinoindolinones and Fluconazole against Candida albicans.

Premachandra Ilandari Dewage Udara Anulal ID   Scott Kevin A KA   Shen Chengtian C   Wang Fuqiang F   Lane Shelley S   Liu Haoping H   Van Vranken David L DL  

ChemMedChem 20150812 10

A spiroindolinone, (1S,3R,3aR,6aS)-1-benzyl-6'-chloro-5-(4-fluorophenyl)-7'-methylspiro[1,2,3a,6a-tetrahydropyrrolo[3,4-c]pyrrole-3,3'-1H-indole]-2',4,6-trione, was previously reported to enhance the antifungal effect of fluconazole against Candida albicans. A diastereomer of this compound was synthesized, along with various analogues. Many of the compounds were shown to enhance the antifungal effect of fluconazole against C. albicans, some with exquisite potency. One spirocyclic piperazine deri  ...[more]

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