Persicamidines—Unprecedented Sesquarterpenoids with Potent Antiviral Bioactivity against Coronaviruses

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.     

Thermolysis of Geminal Diazido Malonamides: Simple Access to Tetrazoles and Functionalization of In Situ Formed Isocyanates

In recent years, the development of synthetic methods to afford nitrogen-containing heterocycles has become increasingly popular. Among these, tetrazoles – an important class of aromatic heterocycles – are of significant interest for example, in medicinal chemistry serving as important bioisosteres. Herein, we present a method to easily access C-substituted tetrazoles via thermolysis of geminal diazido malonamides. Formation and functionalization of in situ formed isocyanates and corresponding reactions were also studied.     

Effects on the pigment distribution in paint formulations

Modern water-borne paints are applied in different areas ranging from high-gloss lacquers to flat, scrub-resistant interior paints. The pigment volume concentration (PVC) is one key-parameter adjusting the application properties. In this work formulations differing in the type of binder and dispersing agent were investigated by various techniques concerning the distribution of pigments in the liquid paints and films. The structure of the paints was analyzed by Remission Light Spectroscopy (RLS), Disc Centrifugation, Cryo-Replica Transmission Electron Microscopy (Cryo-TEM) and Cryo-Scanning Electron Microscopy (Cryo-SEM). The pigment distribution in the films was examined by means of Atomic Force Microscopy (AFM), TEM and RLS. The tendency of the pigments to form aggregates was found to depend on both: the type of binder and the dispersing agent. Only by adjusting the properties of the binder in combination with common dispersants it is possible to get well distributed TiO₂ particles within the paint. Correlation of application properties e.g. gloss and blocking to the microscopic structure is presented.