M. Delpoeta et al., IN-VITRO ANTIFUNGAL ACTIVITIES OF A SERIES OF DICATION-SUBSTITUTED CARBAZOLES, FURANS, AND BENZIMIDAZOLES, Antimicrobial agents and chemotherapy, 42(10), 1998, pp. 2503-2510
Aromatic dicationic compounds possess antimicrobial activity against a
wide range of eucaryotic pathogens, and in the present study an exami
nation of the structures-functions of a series of compounds against fu
ngi was performed, Sixty-seven dicationic molecules were screened for
their inhibitory and fungicidal activities against Candida albicans an
d Cryptococcus neoformans. The MICs of a large number of compounds wer
e comparable to those of the standard antifungal drugs amphotericin B
and fluconazole. Unlike fluconazole, potent inhibitory compounds in th
is series were found to have excellent fungicidal activities. The MIC
of one of the most potent compounds against C, albicans was 0.39 mu g/
ml, and it was the most potent compound against C, neoformans (MIC, le
ss than or equal to 0.09 mu g/ml). Selected compounds were also found
to be active against Aspergillus fumigatus, Fusarium solani, Candida s
pecies other than C, albicans, and fluconazole-resistant strains of C,
albicans and C, neoformans. Since some of these compounds have been s
afely given to animals, these classes of molecules have the potential
to be developed as antifungal agents.