title: Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
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.
authors: Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via Alcide de Gasperi 2, I-53100 Siena, Italy.
authors: Fabrizio
authors: F
authors: Manetti
authors: Daniele
authors: D
authors: Castagnolo
authors: Francesco
authors: F
authors: Raffi
authors: Alessandra T
authors: AT
authors: Zizzari
authors: Suvi
authors: S
authors: Rajamäki
authors: Silvia
authors: S
authors: D'Arezzo
authors: Paolo
authors: P
authors: Visca
authors: Alessandra
authors: A
authors: Cona
authors: Maria Enrica
authors: ME
authors: Fracasso
authors: Denise
authors: D
authors: Doria
authors: Brunella
authors: B
authors: Posteraro
authors: Maurizio
authors: M
authors: Sanguinetti
authors: Giovanni
authors: G
authors: Fadda
authors: Maurizio
authors: M
authors: Botta
mesh_terms: 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
chemical_list: D000935:Antifungal Agents; D047028:Macrocyclic Compounds; C029280:guanidine carboxamide; D014508:Urea; D019791:Guanidine