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 method was developed for the diversification of Meridianin alkaloid in a time and step efficient manner. A wide range of substituents were successfully incorporated, leading to moderate to high product yields and the first synthesis of Meridianin B. This simple method enables the rapid construction of a Meridianin derivative library for antibiofilm evaluation. Preliminary results demonstrate the ability of Meridianin derivatives to inhibit Acinetobacter baumannii biofilms and synergistically lower the antibiotic MIC.