1. 2-Acylhydrazino-5-arylpyrrole derivatives: synthesis and antifungal activity evaluation.
- Author
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Onnis V, De Logu A, Cocco MT, Fadda R, Meleddu R, and Congiu C
- Subjects
- Candida classification, Candida drug effects, Humans, Magnetic Resonance Spectroscopy, Microbial Sensitivity Tests, Species Specificity, Antifungal Agents chemical synthesis, Antifungal Agents pharmacology, Pyrroles chemical synthesis, Pyrroles pharmacology
- Abstract
The synthesis and antifungal activity of 2-acylhydrazino-5-arylpyrroles 21-62 are described. Pyrrole derivatives 21-62 were evaluated for their antifungal activity towards Candida albicans ATCC 10231 and three Candida non-albicans isolated from clinical specimens. Most of them showed very good antifungal activities against Candidae, having MIC values in the 0.39-3.12 microg/mL range and enhanced inhibition potency as compared to that of fluconazole. In addition, some of the most active compounds were tested for cytotoxic activities against breast (MCF-7), lung (H-460), and central nervous system (SF-268) human cancer cell lines with the NCI anticancer drug screen. The activity of pyrroles described in this paper, along with the low toxicity, shows promise for the future development of non-toxic new antimycotic agents. The relationship between functional group variation and biological activity of the evaluated compounds is also discussed.
- Published
- 2009
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