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  • Title: Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
    Author: Manetti F, Castagnolo D, Raffi F, Zizzari AT, Rajamäki S, D'Arezzo S, Visca P, Cona A, Fracasso ME, Doria D, Posteraro B, Sanguinetti M, Fadda G, Botta M.
    Journal: J Med Chem; 2009 Dec 10; 52(23):7376-9. PubMed ID: 19650630.
    Abstract:
    New linear and cyclic guanidines were synthesized and tested in vitro for their antifungal activity toward clinically relevant strains of Candida species, in comparison to fluconazole. Macrocyclic compounds showed a minimum inhibitory concentration in the micromolar range and a biological activity profile in some cases better than that of fluconazole. One macrocyclic derivative was also tested against Aspergillus species and showed high antifungal activity comparable to that of amphotericin B and itraconazole.
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