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. © 2009 American Chemical Society.
Manetti, F., Castagnolo, D., Raffi, F., Zizzari, A.T., Rajamaki, S., D'Arezzo, S., et al. (2009). Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp. JOURNAL OF MEDICINAL CHEMISTRY, 52(23), 7376-7379 [10.1021/jm900760k].