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设计,合成和生物活性评估的三醇抗真菌药物与phenylthiophene结构

Xudong Wu¹, Jiachen Zhang¹, Rongrong Liu¹

¹Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, China.

Bioorganic chemistry

|September 10, 2024

概括

新的三醇抗真菌化合物被开发用于对抗侵入性真菌感染. 化合物19g对常见真菌和抗可纳菌株表现出强烈的活性,显示出治疗严重感染的前景.

科学领域:

药用化学医学化学
菌类学菌类学是指菌类学.
药理学药理学是指药理学的学科.

背景情况:

侵袭性真菌感染由于高发病率和死亡率,对全球健康构成重大风险.
现有的抗真菌疗法面临着耐药性和毒性方面的挑战.
新型抗真菌剂的开发对于有效的疾病管理至关重要.

研究的目的:

为了合成和评估新型的三醇抗真菌衍生品与一个phenylthiophene骨干.
识别有效抗常见和耐药的真菌病原体的强效化合物.
研究有希望的抗真菌候选物的体外和体内特性.

主要方法:

基于基基架的三醇衍生物的合成,使用约迪可纳作为化合物.
抗真菌敏感性测试,包括对Candida albicans,Cryptococcus neoformans和Aspergillus物种的最小抑制度 (MIC80) 的确定.
对抗富可纳抗性真菌菌株的活性评估.
在体外测试人类肝脏微小体稳定性和细胞染色体P450 (CYP) 酶抑制.
评估化合物对正常和癌症人类细胞系的影响.
对化合物19g对Candida albicans丝状和醇成分的影响分析.

主要成果:

一系列的三醇抗真菌衍生物被成功合成.
化合物19g在Candida albicans,Cryptococcus neoformans和Aspergillus的体外表现出强大的抗真菌活性,MIC80为0.0625μg/mL.
化合物19e,19f,19g,19h,19i和19k对抗可纳耐药菌株表现出活性,MIC80值在0.0625至32μg/mL之间.
化合物19g在体外表现出良好的代谢稳定性和CYP酶抑制概况.
化合物19g抑制了Candida albicans的丝状结构,并改变了真菌菌的组成,这表明了特定的作用机制.

结论:

新型基于甲的三醇衍生物代表了一类有前途的抗真菌剂.
化合物19g在治疗侵入性真菌感染方面具有显著的潜力,包括对现有疗法的耐药性.
对化合物19g的作用机制和治疗疗效的进一步研究是有必要的.

关键词:

它具有抗真菌活性,具有抗真菌活性.在CYP51的研究中,国际货币基金组织 (IFI) 是一个国际货币基金组织.代谢稳定性代谢稳定性这种药物是三醇.

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