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Synthesis, antifungal and cytotoxic activities of 2-aryl-3-((piperidin-1-yl)ethyl)thiazolidinones.

Abstract：

:A series of sixteen novel thiazolidinone derivatives were synthesized from the efficient one-pot reaction of 2-(piperidin-1-yl)ethylamine, arenealdehydes and mercaptoacetic acid in good yields. Identification and characterization of products were achieved by NMR and GC-MS techniques. The in vitro antifungal activities of all synthesized compounds were evaluated against seven fungi: Candida albicans, Candida parapsilosis, Candida guilliermondii, Cryptococcus laurentii, Geotrichum sp, Trichosporon asahii and Rhodotorula sp. The results are expressed as the Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC) and the best results were found against the Rhodotorula sp yeast. Two thiazolidinones (4h and 4l), MIC and MFC (16.5 μg/mL) proved to be 1.6 times more active than fluconazole and four of them (4b, 4e, 4g and 4k (MIC and MFC 25 μg/mL)) showed similar activity of standard drug to Rhodotorula sp. In addition, the cytotoxicity of thiazolidinones 4a-p was evaluated on cultured Vero cells and most of them displayed low toxicity (above 98 μg/mL). These preliminary and important results could be considered a starting point for the development of new antifungal agents.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Kunzler A,Neuenfeldt PD,das Neves AM,Pereira CM,Marques GH,Nascente PS,Fernandes MH,Hübner SO,Cunico W

doi

10.1016/j.ejmech.2013.03.030

subject

Has Abstract

pub_date

2013-06-01 00:00:00

pages

74-80

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00190-6

journal_volume

64

pub_type

杂志文章

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