通过氧化循环反应获得替代的三循环异构及其抗真菌性能
Rehema Nakiwala1, Noopur Dasgupta2, Rebecca Wilson2
1Department of Chemistry, 107 Physical Sciences, Oklahoma State University, Stillwater, OK 74078, USA.
合成了新的抗真菌剂,包括新的含硫三醇和[4,5][2,3-c][1,2,4]三醇. 这些化合物对Candida albicans和Trichosporon asahii表现出适度的抗真菌活性.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 抗菌研究 抗菌研究
背景情况:
- 抗真菌药物耐药性的增加需要开发新的抗真菌药物.
- 真菌感染对公众健康构成重大和日益增长的威胁.
研究的目的:
- 合成新型C3,N4替代的三醇衍生物及其相应的佐[4,5]亚[2,3-c][1,2,4]三醇类似物.
- 评估合成化合物对关键真菌病原体的抗真菌活性.
主要方法:
- 合成含有N4 - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - 甲基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基基
- 脱保护以产生自由的醇类似物,然后进行氧化循环形成佐[4,5]亚[2,3-c][1,2,4]三醇.
- 对Candida albicans (SC5314) 和Trichosporon asahii (OK01) 的抗真菌敏感性测试.
主要成果:
- 成功合成了一系列新型含硫三醇和[4,5][2,3-c][1,2,4]三醇,具有广泛的功能组耐受性.
- 机理学研究表明,氧化循环的离子路径涉及二硫化中间体,由酸性条件加速.
- 大多数合成的化合物对Candida albicans和Trichosporon asahii都表现出抗真菌活性.
结论:
- 有效合成了一种新的含硫三醇和化佐[4,5]亚[2,3-c][1,2,4]三醇的新类.
- 新型化合物显示出作为潜在的抗真菌剂的前景,对临床相关的真菌表现出适度的活性.
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