For the first time, derivatives of 3,7-diazabicyclo[3.3.1]nonane (bispidine) were proposed as potential inhibitors of the SARS-CoV-2 main viral protease (3-chymotrypsin-like, 3CLpro). Based on the created pharmacophore model of the active site of the protease, a group of compounds were modeled and tested for activity against 3CLpro. The 3CLpro activity was measured using the fluorogenic substrate Dabcyl-VNSTLQSGLRK(FAM)MA; the efficiency of the proposed approach was confirmed by comparison with literature data for ebselen and disulfiram. The results of the experiments performed with bispidine compounds showed that 14 compounds exhibited activity in the concentration range 1–10 μM, and 3 samples exhibited submicromolar activity. The structure–activity relationship studies showed that the molecules containing a carbonyl group in the ninth position of the bicycle exhibited the maximum activity. Based on the experimental and theoretical results obtained, further directions for the development of this topic were proposed.

Natural leathers (split, velour split, nubuck) ware investigated. Solution of fluorine silane in ethanol was applied as the hydrophobic agent. It is shown that the microstructure of the leather surface, provided its structural elements possess hydrophilic properties, determines the wetting regime and duration of the induction period of changeover from heterogeneous to homogeneous wetting. The heterogeneous regime of wetting is distinguished by low rates of spreading and absorbing. The homogeneous wetting is characterized by high rates of spreading and absorbing of a water drop. A necessary condition of the stable heterogeneous wetting regime and achieving hydrophobicity of leather with structurally inhomogeneous face layer is to preserve the microstructure features of their surface at hydrophobic treatment. The morphological peculiarities of split and ground leather ensure stable hydrophobic properties after application of efficient hydrophobizators.

Sorption and surface properties study of the first three generations of polypyridylphenylene dendrimers.

Careful selection of organic and inorganic components allowed to produce unusual structural types with promising practical properties by facile syntheses. In this paper, we describe novel supramolecular architectures comprising organic...