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发现了具有针对耐药性Mycobacterium结核病的选择性活性的超短β-peptoids

John Kauffman¹, Jake Cuevas¹, Janaya Feiner¹

¹Chemistry Department, Wheaton College, 501 College Ave, Wheaton, IL 60187, United States.

European journal of medicinal chemistry

|March 27, 2025

概括

新的类药物显示出作为抗肺结核药物的前景. 研究人员开发并选了22种化合物,其中有两个强有力的候选者,JC5和MM2,证明了对耐药性Mycobacterium结核病菌株的有效性.

科学领域:

药用化学医学化学
药物发现药物发现药物发现
结核病研究结核病研究

背景情况:

迫切需要新型抗结核病 (抗结核病) 药物,这是由于Mycobacterium tuberculosis (M.tb) 的抗药性增加.
与抗微生物 (AMP) 相比,Oligo-N替代的甘氨酸 (类) 具有优势,包括增强的稳定性,蛋白酶抵抗性,成本效益和药物适用性.

研究的目的:

设计,合成和选新的alpha-和beta-peptoids用于抗结核病活性.
为了识别针对药物敏感和耐药的M.tb菌株的强有力的类候选者.

主要方法:

选22个合成的α和β-peptoids对M.tb菌株H37Rv使用微板Alamar蓝色试验 (MABA).
确定有前途的化合物的最小抑制度 (MIC) 和最小杀菌度 (MBC).
对巨细胞的细胞内活性和对维罗细胞的选择性进行评估.

主要成果:

八种类的MIC低于10微克/毫升,其中JC5 (1.48微克/毫升) 和MM2 (2.97微克/毫升) 是最强的.
JC5和MM2保留了对异化和利法抗性M.tb菌株和全球类代表的活性.
这两种化合物都表现出细胞内活性 (EC90 < 10μg/ml) 和具有适度选择性的窄谱活性.

结论:

阿尔法和β-类化合物是开发新的抗结核病疗法的一类有希望的化合物.
JC5和MM2被确定为用于进一步开发抗结核药物的强化合物.

关键词:

抗结核病剂是一种抗结核病剂.抗微生物 (AMP) 是一种抗微生物.耐药性M.T.B.T. 的药物.菌根细菌 (Mycobacteria) 是一种细菌.类蛋白质 (peptoids) 是一种蛋白质.

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