IN-VITRO ANTIFUNGAL ACTIVITIES OF A SERIES OF DICATION-SUBSTITUTED CARBAZOLES, FURANS, AND BENZIMIDAZOLES

Citation
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
Citations number
32
Categorie Soggetti
Pharmacology & Pharmacy",Microbiology
ISSN journal
00664804
Volume
42
Issue
10
Year of publication
1998
Pages
2503 - 2510
Database
ISI
SICI code
0066-4804(1998)42:10<2503:IAAOAS>2.0.ZU;2-Y
Abstract
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.