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对沙利西尔化衍生物进行临床前试验,以探索其作为新抗结核剂的潜力

Andressa Lorena Ieque¹, Carolina Trevisolli Palomo¹, Vitória Gabriela de Freitas Spanhol¹

¹Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Paraná, 87020-900, Brazil.

Tuberculosis (Edinburgh, Scotland)

|July 30, 2024

概括

这项研究合成了22种基,确定了化合物18作为一个有前途的抗结核病药物候选物,具有较低的最小抑制度和较低的抗结核菌细胞毒性.

科学领域:

药用化学医学化学
药物发现药物发现药物发现
抗菌剂抗菌剂抗菌剂

背景情况:

结核病 (TB) 仍然是一个全球卫生挑战.
开发新的抗结核病药物对于对抗耐药菌株至关重要.
Salicylhydrazones 是一类具有潜在生物活性的化合物.

研究的目的:

为了合成22种沙利基化衍生物.
评估它们作为抗结核病原型药物的体外潜力.
为了确定针对Mycobacterium结核病的新型候选药物.

主要方法:

合成22种沙利基化衍生物.
对Mtb H37Rv和临床分离物进行最小抑制度 (MIC) 测试.
进行了药物组合,细胞毒性,乙基化物积累测定和in silico ADMET分析.

主要成果:

化合物18对Mtb H37Rv.表现出最低的MIC (0.49微克/毫升).
化合物10,11和18对药物敏感和耐药的临床隔离物表现出活性.
化合物18表现出高选择性 (SI高达4,205),具有有前途的细胞毒性概况.

结论:

基原衍生物显示出作为抗结核病药物的显著潜力.
化合物18是有前途的候选物,因为它具有强大的活性和有利的安全性.
对这些化合物的进一步研究可能会导致新的结核病疗法.

关键词:

细胞毒性细胞毒性药物发现药物发现这是一种Mycobacterium tuberculosis的细菌.Salicylhydrazones 的使用方法

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