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新的循环阿里尔瓜尼丁基架作为开发抗菌和抗病毒剂的平台

Przemysław Zaręba¹, Anna K Drabczyk², Sylwia Wnorowska³

¹Faculty of Chemical Engineering and Technology, Department of Chemical Technology and Environmental Analytics, Cracow University of Technology, 24 Warszawska Street, 31-155 Cracow, Poland.

Bioorganic chemistry

|July 20, 2023

概括

新的循环阿里尔瓜尼丁化合物显示出强大的抗微生物和抗病毒活性,对抗危险的病原体,如金黄色葡萄球菌和SARS-CoV-2. 这些新型分子具有低毒性,在对抗传染病方面具有有前途的治疗潜力.

科学领域:

药用化学医学化学
有机合成有机合成
抗微生物和抗病毒研究.

背景情况:

传染病仍然是全球主要的健康威胁,由抗生素耐药性和病毒突变加剧.
迫切需要新的抗微生物和抗病毒药物来应对这些挑战.
循环guanidine部分被认为是开发此类药物的有前途的支架.

研究的目的:

设计,合成和评估新型循环阿里尔瓜尼丁化合物的抗菌和抗病毒活性.
评估最有前途的候选物质的细胞毒性和溶血性质.
为了识别潜在的治疗应用针对传染病的化合物.

主要方法:

分子建模用于化合物设计.
微波 (MW) 和声化学合成方法被用于化合物制备.
针对大肠杆菌 (Escherichia coli),宝曼尼菌 (Acinetobacter baumannii) 假菌 (Pseudomonas aeruginosa) 黄金菌 (Staphylococcus aureus) 菌 (Candida albicans) 和新型菌 (Cryptococcus neoformans) 进行抗菌查.
使用生物发光免疫试验对严重急性呼吸系统综合征冠状病毒2 (SARS-CoV-2) 进行抗病毒查.
对活性化合物进行了细胞毒性和溶血性检测.

主要成果:

化合物12j (N-[2-(纳-1-yl) 乙烯]-5--1,4,5,6-四-1,3,5--2-胺) 显示出对*金黄色葡萄球菌*和*新型菌* (MIC ≤0.25μg/mL) 的显著抑制.
化合物12j没有表现出细胞毒性或溶血效应 (CC50,HC10>32μm/mL).
广泛的数据库揭示了大量活跃的循环阿里格胺分子,大约10%显示高活性 (MIC ≤1 mg/mL).

结论:

新型循环阿里格胺衍生物具有显著的抗微生物和抗病毒潜力.
化合物12j代表了一个有前途的候选人,因为它的高疗效和低毒性.
对这些化合物的进一步研究可能会导致对传染病的新治疗方法的开发.

关键词:

抗菌剂抗菌剂抗菌剂这是一种抗真菌药物.循环的阿里尔瓜尼丁类药物.在RBD:ACE2中.这就是SARS-CoV-2病毒.

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