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设计,合成和评估Pyrazoleacetamide衍生物的抗真菌活性
Onkar G Kachi1, Hari R Pawar1, Anuruddha R Chabukswar2
1Department of Chemistry, MES Abasaheb Garware College, Karve Road, Pune, 411 004, India.
Medicinal chemistry (Shariqah (United Arab Emirates))
|June 13, 2024
概括
新的皮拉衍生物对Candida albicans和Aspergillus niger具有强大的抗真菌活性. 这些化合物为现有治疗提供了有希望的替代方案,解决了真菌感染中耐药性和毒性问题.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 计算化学计算化学
背景情况:
- 真菌感染带来了重大治疗挑战,药物耐药性和毒性加剧了这一问题.
- 随着COVID-19的流行,人们迫切需要新型抗真菌剂.
- 开发新的药物分子对于管理新兴传染病至关重要.
研究的目的:
- 设计使用分子建模针对目标1EA1.1的新型pyrazole衍生物.
- 通过多步骤的方法合成十种pyrazole衍生物.
- 评估合成化合物的抗真菌潜力.
主要方法:
- 使用常规有机方法合成pyrazole衍生物.
- 使用FT-IR,1HNMR,13CNMR和LC-MS合成的分子的表征.
- 在体外对Candida albicans和Aspergillus niger的抗真菌活性进行评估.
主要成果:
- 两种化合物,OK-7和OK-8,与目标蛋白1EA1.1呈现出显著的对接相互作用.
- OK-7和OK-8在体外表现出强大的抗真菌活性,对抗白 Candida albicans 和 Aspergillus niger.
- 对OK-7和OK-8的最小抑制度 (MIC) 确定为50μg/ml.
结论:
- 含有-CH3,CH3O-和-CN组的皮拉衍生物显示出显著的抗真菌活性.
- 这些化合物代表了开发新抗真菌药物的潜在候选者.
- 对于药物化学应用,需要进一步探索这些皮拉衍生物.
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