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.

Non-leaching antimicrobial biodegradable PBAT films through a facile and novel approach

“…Guanidine-based cationic polymers show excellent anti-bacterial [19][20][21][22], anti-fungal [23], and anti-viral activities [24][25][26]. More importantly, it has been noted that guanidine-based polymers can overcome bacterial resistance [27,28].…”

Guanidines from ‘toxic substances’ to compounds with multiple biological applications – Detailed outlook on synthetic procedures employed for the synthesis of guanidines

“…One macrocyclic derivative tested against Aspergillus species showed high antifungal activity comparable to that of amphotericin B and itraconazole. [187] 3.5.6. Anticonvulsant Activity…”

Synthesis, Characterization and Biological Activity of Novel Zirconium, Zinc and Cadmium Complexes Derived from Substituted Tetramethyl Guanidine

“…Guanidine, has already gained excessive attention since its discovery, due to their chemical and biological properties (Manetti et al, 2009). They also appear in a number of important antibiotic drugs including: Streptomycin, Trimethoprim, Chlorhexidine, Polyhexamethylene bi guanidine, Pyrrplidine bis-cyclic guanidine and others (Ghulam Murtaza, 2012).…”