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Direct modifications of the cyclic peptide Polymyxin B leading to analogues with enhanced in vitro antibacterial activity.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-03-30 , DOI: 10.1016/j.bmcl.2020.127163 Pamela Brown 1 , Omar Abdulle 2 , Steven Boakes 2 , Esther Duperchy 2 , Stephen Moss 3 , Mona Simonovic 2 , Steven Stanway 3 , Antoinette Wilson 3 , Michael J Dawson 1
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-03-30 , DOI: 10.1016/j.bmcl.2020.127163 Pamela Brown 1 , Omar Abdulle 2 , Steven Boakes 2 , Esther Duperchy 2 , Stephen Moss 3 , Mona Simonovic 2 , Steven Stanway 3 , Antoinette Wilson 3 , Michael J Dawson 1
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Synthetic modifications have been made directly to the cyclic peptide core of polymyxin B, enabling the further understanding of structure activity relationships of this antimicrobial peptide. Such modified polymyxins are also substrates for enzymic hydrolysis, enabling the synthesis of a variety of semi-synthetic analogues, resulting in compounds with increased in vitro antibacterial activity.
中文翻译：
环肽多粘菌素B的直接修饰导致体外抗菌活性增强的类似物。
已经直接对多粘菌素B的环状肽核心进行了合成修饰，从而可以进一步了解这种抗菌肽的结构活性关系。此类修饰的多粘菌素还是酶水解的底物，能够合成多种半合成类似物，从而使化合物具有更高的体外抗菌活性。
更新日期：2020-04-20
中文翻译：
环肽多粘菌素B的直接修饰导致体外抗菌活性增强的类似物。
已经直接对多粘菌素B的环状肽核心进行了合成修饰，从而可以进一步了解这种抗菌肽的结构活性关系。此类修饰的多粘菌素还是酶水解的底物，能够合成多种半合成类似物，从而使化合物具有更高的体外抗菌活性。
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