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作为有前途的抗结核和抗菌剂的 furan-thiazole 基架:合成,表征,生物评估和计算分析
Yuvraj R Sable1,2, Rahul A Shinde3, Haya Khader Ahmad Yasin4,5
1Research Centre in Chemistry, Mahatma Gandhi Vidyamandir's Loknete Vyankatrao Hiray Arts, Science and Commerce College Panchavati Nashik 422003 Maharashtra India sabley70@gmail.com vishnuadole86@gmail.com.
RSC advances
|August 27, 2025
概括
新的 furan-thiazole 水衍生物显示为结核病和细菌感染的新疗法. 化合物4a-4c对Mycobacterium结核病有效,而4g对黄金菌和大肠杆菌具有强烈的抗菌活性.
科学领域:
- 医学化学
- 有机合成
- 发现抗菌药物
背景情况:
- 结核病和细菌感染仍然是全球严重的健康威胁.
- 持续需要新型治疗药物以提高疗效和降低耐药性.
- furan-thiazole 支架在药物化学应用中已经显示出潜力.
研究的目的:
- 合成和表征一系列的 furan-thiazole 衍生物.
- 评估合成化合物的抗结核和抗菌活性.
- 通过计算研究研究结构-活动关系和结合机制.
主要方法:
- 使用光谱技术 (FT-IR,NMR,HRMS) 合成和表征-硫衍生物 (4a-4n).
- 在体外对结核菌H37Rv,金黄色葡萄球菌和大肠杆菌进行抗菌检测.
- 针对关键酶的分子对接研究和体ADME/DFT分析.
主要成果:
- 化合物4a,4b和4c表现出显著的抗结核活性 (MIC = 3. 12μg mL-1),相当于皮拉津胺.
- 化合物4g具有强烈的抗菌活性,抑制区为19毫米 (黄金色细菌) 和17毫米 (大肠杆菌).
- 分子对接显示了与M. 结核病CYP51和大肠杆菌2,2-二甲基甘氨酸脱碳酶的强烈结合亲和性,得到了在中ADME和DFT的良好支持.
结论:
- 黄酸衍生物4a,4b和4c是抗结核药物开发的有希望的候选药物.
- 化合物4f和4g具有作为有效抗菌剂的潜力.
- 这项研究为进一步优化和开发这些化合物的新型抗菌疗法提供了基础.
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