Chemistry, School of Forensic and Investigative Sciences, University of Central Lancashire, Preston PR1 2HE, UK.
Eur J Med Chem. 2013 Jun;64:222-7. doi: 10.1016/j.ejmech.2013.03.031. Epub 2013 Apr 6.
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.
本文报道了多种 N-烷基化 2,3,3-三甲基吲哚啉和 2-甲基苯并噻唑的合成。通过初步筛选对酿酒酵母（Saccharomyces cerevisiae）、裂殖酵母（Schizosaccharomyces pombe）和白色念珠菌（Candida albicans）进行评估，研究了它们作为抗真菌剂的潜力。统计分析表明，链长与酿酒酵母和裂殖酵母的生长抑制之间存在很强的关系（每种情况下 p < 0.0001）。特别有趣的是，这两组化合物对酿酒酵母的活性，因为它正在成为一种机会性病原体，尤其是在免疫抑制和免疫功能低下的患者中。建立了生物测定来比较我们一系列 N-烷基化化合物与经典抗真菌药物两性霉素 B 和噻苯达唑的疗效。
