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新型醇替代的1,3,4-氧沙醇衍生物:设计,合成,抗菌和抗炎潜力

Vishal Sharma¹, Rina Das¹, Dinesh Kumar Mehta²

¹Department of Pharmaceutical Chemistry, MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, 133207, India.

Molecular diversity

|August 3, 2024

概括

新型诺龙-氧迪亚醇杂交物显示出强大的抗菌和抗炎活性. 这些新化合物对关键细菌菌株有效,具有有前途的治疗潜力,特别是作为COX-II抑制剂.

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:

耐药细菌的出现需要开发新的抗菌剂.
昆和1,3,4-氧沙醇支架因其多样化的生物活性而得到认可.
药的混合化是一种提高疗效和扩大活性谱的策略.

研究的目的:

设计和合成新的诺替代的1,3,4-氧沙衍生物.
评估合成的化合物的抗菌,抗真菌和抗炎作用.
研究这些杂交物作为循环氧化酶-2 (COX-II) 抑制剂的潜力.

主要方法:

合成使用pipemidic酸作为基础的奇诺隆-氧迪亚醇衍生物.
通过IR,1H NMR和质谱学来阐明合成化合物的结构.
在体外评估抗菌活性对抗阳性和阴性细菌,以及抗真菌活性对抗Candida albicans.
在体外通过COX-II抑制试验评估抗炎活性.
分子对接研究,以预测与DNA回转酶酶的结合相互作用.

主要成果:

所有合成的奇诺隆-氧沙醇衍生物 (4a-l) 在结构上都得到了确认.
化合物4f,4h和4k表现出显著的宽谱抗菌活性 (MIC 8μg/mL),在测试菌株中表现优于西普洛素,除了Enterococcus faecalis.
合成的化合物对Candida albicans的抗真菌活性有限.
化合物4k表现出高百分比的对COX-II的抑制,这表明它具有抗炎性潜力.
对接研究揭示了DNA旋转酶活性口袋内化合物4f,4h和4k的强有力的结合相互作用,结合能量优于参考配体.

结论:

这种新型的诺-氧沙醇杂交物具有显著的抗菌和抗炎性质.
化合物4f,4h和4k被确定为进一步开发抗菌剂和COX-II抑制剂的主要候选物.
这项研究强调了与1,3,4-oxadiazole混合化pipemidic酸的潜力,以发现新的治疗剂.

关键词:

一,三,四氧沙醇抗炎药物抗炎药物抗炎药物抗微生物药物抗微生物药物结合能量是有约束力的.皮佩米迪酸是指皮佩米迪酸.昆诺隆 (quinolone) 是一种氨酸.

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