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Tyler, Andrew R, Okoh, Adeyi Okoh, Lawrence, Clare Louise 
ORCID: 0000-0003-0170-0079, Jones, Vicky Claire ORCID: 0000-0001-8401-5223, Moffatt, Colin and Smith, Robert B ORCID: 0000-0002-2829-5360
(2013)
N-Alkylated 2,3,3-trimethylindolenines and 2-methylbenzothiazoles. Potential lead compounds in the fight against Saccharomyces cerevisiae infections.
European journal of medicinal chemistry, 64
.
pp. 222-227.
ISSN 1768-3254
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Official URL: http://dx.doi.org/10.1016/j.ejmech.2013.03.031
Abstract
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.
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