一些新的二皮里米丁衍生物的合成,表征和生物特征
Madiha Kanwal1, Humaira Nadeem1, Sumra Malik1
1Department of Pharmaceutical Chemistry, Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad, Pakistan, 44000.
Heliyon
|January 15, 2025
概括
新的二皮里米丁衍生物显示出强大的抗微生物和抗炎性质,为对抗耐药性感染和炎症提供了一个有希望的,无毒的替代品.
科学领域:
- 药用化学 医学化学
- 药理学 药理学是指药理学的学科.
- 药物发现 药物发现 药物发现
背景情况:
- 越来越多的抗药性 (MDR) 病原体的流行需要开发新的抗菌剂.
- 由于交叉耐药性,现有的治疗方法面临挑战,突出显示出需要具有独特作用机制的化合物.
研究的目的:
- 为了合成新的二皮里米丁衍生物.
- 评估它们的抗微生物,抗炎和抗氧化活性.
- 通过细胞毒性研究来评估它们的安全性.
主要方法:
- 合成的二皮里米丁衍生物的光谱表征 (1H NMR,FT-IR).
- 使用AutoDock Vina对抗细菌和真菌蛋白质点的分子对接研究.
- 在体外评估抗微生物,抗氧化剂和抗炎活性.
- 在体内评估抗炎作用,使用卡拉基南诱导的后脚胀模型.
- 使用MTT测定进行体外细胞毒性评估.
主要成果:
- 所有合成的衍生品都通过光谱检测得到了证实.
- 化合物对目标蛋白具有显著的结合亲和力,4c化合物表现出强大的抗菌活性 (-10 kcal/mol),4b化合物表现出强大的抗真菌潜力 (-10.8 kcal/mol).
- 化合物4a,4b和4c表现出显著的抗菌活性对细菌细菌和抗真菌活性对 Candida glabrata.
- 化合物4b表现出显著的抗氧化活性 (63.85±1.39),而化合物4a和4b显示出有前途的抗炎作用.
- 选择的衍生品表现出良好的安全性,细胞存活率高 (99%和98%).
结论:
- 新合成的二皮里米丁衍生物具有显著的抗微生物和抗炎性质.
- 这些化合物有效地向耐药菌株和炎症通路.
- 这些衍生品呈现出无毒的特征,表明它们作为安全有效的治疗剂的潜力.
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