Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
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.
Manetti
Fabrizio
F
Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via Alcide de Gasperi 2, I-53100 Siena, Italy.
Castagnolo
Daniele
D
Raffi
Francesco
F
Zizzari
Alessandra T
AT
Rajamäki
Suvi
S
D'Arezzo
Silvia
S
Visca
Paolo
P
Cona
Alessandra
A
Fracasso
Maria Enrica
ME
Doria
Denise
D
Posteraro
Brunella
B
Sanguinetti
Maurizio
M
Fadda
Giovanni
G
Botta
Maurizio
M
D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001230:Aspergillus / Q000187:drug effects*; D002175:Candida / Q000187:drug effects*; D015195:Drug Design; D019791:Guanidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D047028:Macrocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D000935:Antifungal Agents; D047028:Macrocyclic Compounds; C029280:guanidine carboxamide; D014508:Urea; D019791:Guanidine