An Efficient Synthesis of 3-Alkylpyridine Alkaloids Enables Their Biological Evaluation

ChemMedChem. 2021 Mar 23. doi: 10.1002/cmdc.202100134. Online ahead of print.


3-Alkylpyridine alkaloids (3-APAs) isolated from the arctic sponge Haliclona viscosa represent a promising group of bioactive marine alkaloids. However, due to limited bioavailability, investigations of their bioactivity have been limited. Additionally, synthesis of a common intermediate requires the use of protecting groups and harsh conditions. In this work, we developed a simple and concise 2-step route to 9 different natural and synthetic haliclocyclins. These compounds displayed modest antibiotic activity against several Gram-positive bacterial strains.

PMID:33755337 | DOI:10.1002/cmdc.202100134