Total and Semisyntheses of Polymyxin Analogues with 2-Thr or 10-Thr Modifications to Decipher the Structure–Activity Relationship and Improve the Antibacterial Activity
Jian Li, Dongliang Guan, Feifei Chen, Weiwei Shi, Lefu Lan, Weitong Huang
Abstract
exhibited 2-8-fold higher activity against different strains and lower toxicity toward the HK-2 cell line. This work explored the SAR of polymyxin 2-/10-Thr and provided a promising strategy for the development of novel polymyxin derivatives.
Topics & Concepts
ChemistryPolymyxinAntibacterial activityStructure–activity relationshipBacteriaIn vitroPseudomonas aeruginosaPolymyxin BChemical synthesisBiological activityBiochemistryAntibacterial agentCombinatorial chemistryAntibioticsStereochemistryBiologyGeneticsAntibiotic Resistance in BacteriaAntibiotics Pharmacokinetics and EfficacyPhenothiazines and Benzothiazines Synthesis and Activities