Protecting-Group-Free Synthesis of Meridianin A-G and Derivatives and Its Antibiofilm Evaluation

Herein, a protecting-group-free protocol was developed to realize a time and step economy diversification of the Meridianin alkaloid. A broad range of substituents are tolerated to deliver the products in moderate to high yields, and the first synthesis of Meridianin B was achieved. The simplicity of this protocol enables the rapid construction of a Meridianin derivative library for antibiofilm evaluation. Preliminary results reveal that Meridianin derivatives were capable of inhibiting the Acinetobacter baumannii biofilm and lowering the antibiotic MIC synergistically.

Automated summary

A protecting-group-free protocol was developed for the efficient diversification of the Meridianin alkaloid, leading to the synthesis of Meridianin B. The protocol tolerates a broad range of substituents, resulting in moderate to high product yields. Furthermore, preliminary studies demonstrate the potential of Meridianin derivatives in inhibiting Acinetobacter baumannii biofilm and enhancing antibiotic efficacy.