Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 64, Issue -, Pages 222-227Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.03.031
Keywords
Antifungal; Drug design; 2-Methylbenzothiazole; Structure activity relationship; 2,3,3-Trimethylindolenine; Yeast
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Funding
- Centre for Material Sciences, School of Forensic and Investigative Sciences
- Royal Society of Chemistry (Lancaster and District Section)
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The synthesis of a variety of N-alkylated 2,3,3-trimethylindolenines and 2-methylbenzothiazoles is reported herein. Their potential as antifungal agents is evaluated by preliminary screening against Saccharomyces cerevisiae (S. cerevisiae), Schizosaccharomyces pombe (S. pombe), and Candida albicans (C albicans). Statistical analyses illustrate a strong relationship between chain length and growth inhibition for S. cerevisiae and S. pombe (p < 0.0001 in every case). Of particular interest is the activity of both sets of compounds against S. cerevisiae, as this is emerging as an opportunistic pathogen, especially in immunosuppressed and immunocompromised patients. Bioassays were set up to compare the efficacy of our range of N-alkylated compounds against classic antifungal agents; Amphotericin B and Thiabendazole. (C) 2013 Elsevier Masson SAS. All rights reserved.
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