化学
两亲性
广谱
心环烯
组合化学
抗菌活性
有机化学
膜
细菌
生物化学
分子
生物
共聚物
遗传学
聚合物
作者
Saroj Maji,Sariyah Akhtar,Sabyasachi Halder,I. Chatterjee,Devesh Pratap Verma,Neeraj Verma,Jyotshana Saroj,Deepanshi Saxena,Rahul Maitra,Juhi Sharma,Bhawana Sharma,Hidehiro Sakurai,Kalyan Mitra,Sidharth Chopra,Jimut Kanti Ghosh,Gautam Panda
标识
DOI:10.1021/acs.jmedchem.4c00666
摘要
To date, the use of corannulene has been restricted in the area of material science, but its application in biomedical research has yet to be established due to its nonsolubility in an aqueous environment and synthetic infeasibility. Herein, we detail the development of a new family of highly curved π-conjugated corannulene-containing unnatural α-amino acid (CAA) derivatives to overcome this challenge. These CAAs have been extended as novel constituents for the synthesis of corannulene-containing water-soluble cationic peptides (CCPs), which display inhibitory activity against broad-spectrum pathogenic bacteria along with drug-resistant bacteria via a membrane-damaging mechanism. Importantly, several of the synthesized peptides were found to be appreciably nonhemolytic against hRBCs and noncytotoxic against mammalian 3T3 cells.
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