Abstract
Tuberculosis represents one of the ten most common courses of death worldwide and the emergence of multidrug‐resistant M. tuberculosis makes the discovery of novel anti‐tuberculosis active structures an urgent priority. Here, we show that (+)‐floyocidin B representing the first example of a novel dihydroisoquinoline class of fungus‐derived natural products, displays promising antitubercular hit properties. (+)‐Floyocidin B was identified by activity‐guided extract screening and its structure was unambiguously determined by total synthesis. The absolute configuration was deduced from a key synthesis intermediate by single crystal X‐ray diffraction analysis. A hit series was generated by the isolation of further natural congeners and the synthesis of analogs of (+)‐floyocidin B. Extensive biological and physicochemical profiling of this series revealed first structure‐activity relationships and set the basis for further optimization and development of this novel antitubercular scaffold.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.