Litcius/Paper detail

Persicamidines—Unprecedented Sesquarterpenoids with Potent Antiviral Bioactivity against Coronaviruses

Lena Keller, Emilia Oueis, Amninder Kaur, Nasim Safaei, Susanne H. Kirsch, Antonia P. Gunesch, Sibylle Haid, Ulfert Rand, Luka Čičin‐Šain, Chengzhang Fu, Joachim Wink, Thomas Pietschmann, Rolf Müller

2022Angewandte Chemie International Edition15 citationsDOIOpen Access PDF

Abstract

A new family of highly unusual sesquarterpenoids (persicamidines A-E) exhibiting significant antiviral activity was isolated from a newly discovered actinobacterial strain, Kibdelosporangium persicum sp. nov., collected from a hot desert in Iran. Extensive NMR analysis unraveled a hexacyclic terpenoid molecule with a modified sugar moiety on one side and a highly unusual isourea moiety fused to the terpenoid structure. The structures of the five analogues differed only in the aminoalkyl side chain attached to the isourea moiety. Persicamidines A-E showed potent activity against hCoV-229E and SARS-CoV-2 viruses in the nanomolar range together with very good selectivity indices, making persicamidines promising as starting points for drug development.

Topics & Concepts

MoietyTerpenoidStereochemistryChemistrySide chainTwo-dimensional nuclear magnetic resonance spectroscopySelectivityBiochemistryOrganic chemistryCatalysisPolymerMicrobial Natural Products and BiosynthesisNatural product bioactivities and synthesisCarbohydrate Chemistry and Synthesis