Zhou Yuxin, Liang Xiao-Wei
Jinling High School 169 Zhongshan Road Nanjing Jiangsu 210005 China.
Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South University Changsha 410008 China
RSC Adv. 2021 Nov 24;11(60):37942-37951. doi: 10.1039/d1ra07503a. eCollection 2021 Nov 23.
Antibiotics produced by soil microorganisms have been widespread and have cured the most prevalent diseases since 1940s. However, recent bacterial resistance to existing antibacterial drugs is causing a public health crisis. The structure-activity relationship of antibiotics needs to be established to search for existing antibiotics-based next-generation drug candidates that can conquer the challenge of bacterial resistance preparedness, which relies on the development of highly efficient total synthesis strategies. The solid-phase strategy has become important to circumvent tedious intermediate isolation and purification procedures with simple filtrations. This review will give a brief overview of recent applications of solid-phase strategy in the total synthesis of antibiotics.
土壤微生物产生的抗生素自20世纪40年代以来已广泛应用，并治愈了大多数常见疾病。然而，最近细菌对现有抗菌药物的耐药性正在引发一场公共卫生危机。需要建立抗生素的构效关系，以寻找基于现有抗生素的下一代候选药物，这些药物能够应对细菌耐药性带来的挑战，而这依赖于高效全合成策略的发展。固相策略已变得至关重要，它可以通过简单过滤避免繁琐的中间体分离和纯化过程。本文将简要概述固相策略在抗生素全合成中的最新应用。
