2-Acylhydrazino-5-arylpyrrole derivatives: synthesis and antifungal activity evaluation.
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.
Onnis
Valentina
V
Dipartimento di Tossicologia, Sezione di Chimica Farmaceutica, Università degli Studi di Cagliari, via Ospedale 72, Cagliari I-09124, Italy. vonnis@unica.it
De Logu
Alessandro
A
Cocco
Maria T
MT
Fadda
Roberta
R
Meleddu
Rita
R
Congiu
Cenzo
C
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002175:Candida / Q000145:classification / Q000187:drug effects; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013045:Species Specificity
D000935:Antifungal Agents; D011758:Pyrroles