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Persicamidines—Unprecedented Sesquarterpenoids with Potent Antiviral Bioactivity against Coronaviruses |
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| Authors: | Prof Dr Lena Keller Dr Emilia Oueis Dr Amninder Kaur Dr Nasim Safaei Dr Susanne H Kirsch Dr Antonia P Gunesch Dr Sibylle Haid Dr Ulfert Rand Prof Dr Luka Čičin-Šain Dr Chengzhang Fu PD Dr Joachim Wink Prof Dr Thomas Pietschmann Prof Dr Rolf Müller |
| Institution: | 1. Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Saarland University Campus, 66123 Saarbrücken, Germany;2. Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Saarland University Campus, 66123 Saarbrücken, Germany
German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, 38124 Braunschweig, Germany;3. German Centre for Infection Research (DZIF), Partner Site Hannover-Braunschweig, 38124 Braunschweig, Germany |
| 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. |
| Keywords: | Actinobacteria Antiviral Agents Oleandrose Sesquarterpenes Structure Elucidation |