The Discovery and Structure-Activity Evaluation of (+)-Floyocidin B and Synthetic Analogs.

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 bi

SUBMITTER: Kleiner Y 

PROVIDER: S-EPMC9298916 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature