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Updated: Mar 14, 2026

A Direct, Early Stage Guanidinylation Protocol for the Synthesis of Complex Aminoguanidine-containing Natural Products
Published on: September 9, 2016
New synthetic approaches towards analogues of bedaquiline
Daniel L Priebbenow1, Lisa Barbaro1, Jonathan B Baell1
1Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia. Jonathan.baell@monash.edu.
Abstract:
Multi-drug resistant tuberculosis (MDR-TB) is of growing global concern and threatens to undermine increasing efforts to control the worldwide spread of tuberculosis (TB). Bedaquiline has recently emerged as a new drug developed to specifically treat MDR-TB. Despite being highly effective as a result of its unique mode of action, bedaquiline has been associated with significant toxicities and as such, safety concerns are limiting its clinical use. In order to access pharmaceutical agents that exhibit an improved safety profile for the treatment of MDR-TB, new synthetic pathways to facilitate the preparation of bedaquiline and analogues thereof have been discovered.
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