Kseniya S. Kovaleva's research while affiliated with Novosibirsk Institute of Organic Chemistry and other places

... Since the properties of isatin derivatives as inhibitors of the main viral protease of coronoviruses were previously described in the literature, we performed inhibitors of orthopoxiviruses and influenza viruses [32], these compounds being of particular interest as effective inhibitors of Hantaan viruses causing hemorrhagic fever with renal syndrome, a zoonotic viral disease for which there is currently no effective chemotherapy [33]. An effective and stereoselective method for the synthesis of spiro derivatives based on camphor and fenchone hydrazones has recently been described [34]. ...

... Te elution systems consisting of methanol, acetonitrile, water, and formate water were compared according to the physicochemical properties and the chromatographic behavior of the analytes [20,[22][23][24]. Te results show that the separation efect of methanol-water or acidic water as system components was not ideal, but the optimized separation efect of acetonitrile-water-formic acid system components was better, and each chromatographic peak separation and the theoretical number of trays met the requirements. ...

... We have shown a convenient synthesis of N-heterocyclic compounds by direct alkylation of hydrazones with aliphatic dihalides; the reaction of hydrazones with 1,2-ethanediol in the presence of formaldehyde with the addition of samarium nitrate leads to the formation of compounds containing a 1,5,3-dithioazepane fragment [30]. By the reaction of camphor hydrazone with various isothiacyanates, N-substituted thiosemicarbazones were obtained, on the basis of which a significant set of 2-iminothiazolidine-4-ones and 2,3-dihydrothiazolones were synthesized [31]. Among the described heterocyclic derivatives, compounds active against smallpox vaccine and effective inhibitors of the entry of the Marburg virus were found. ...

... Our research team is actively working in the field of searching for new effective agents with a wide range of antiviral properties based on terpene series compounds [26,27]. It has been shown that the presence of a bicyclic frame fragment is extremely important for the manifestation of antiviral activity [28,29]. A simple and convenient method of introducing an amino group into a natural backbone, suitable for further transformations, is the synthesis of hydrazones from natural ketones. ...

... The binding of stachyflin increases the energy barrier required for this conformational transition and the formation of one α-helix. Another compound, ginsamide (28) [72], exhibiting pronounced activity against influenza virus can bind at the CPH site by contacting V2115. This binding site was selected based on the similarity of the pharmacophoric profiles of camphecene and ginsamide ( Figure 9B) as well as based on the result of sequencing a ginsamide-resistant influenza A virus. ...

... Attractive substance classes for the creation of new TDP1 inhibitors based on them are not only derivatives of dehydroabietic acid, but also other resin acids. Previously, our team obtained ureas with nordehydroabietic 6a-b and norabietic fragments 7a-b in the structure ( Figure 2) [14]. The influence of the type of attachment of the adamantane fragment-in the first or second position of the scaffold-was studied. ...

... Since the properties of isatin derivatives as inhibitors of the main viral protease of coronoviruses were previously described in the literature, we performed inhibitors of orthopoxiviruses and influenza viruses [32], these compounds being of particular interest as effective inhibitors of Hantaan viruses causing hemorrhagic fever with renal syndrome, a zoonotic viral disease for which there is currently no effective chemotherapy [33]. An effective and stereoselective method for the synthesis of spiro derivatives based on camphor and fenchone hydrazones has recently been described [34]. ...

... In a series of dehydroabiethylamine derivatives carrying a 2-iminothiazolidine-4thione or 2-thioxoimidazolidine-4-thione moiety (compounds 59 and 60, Figure 16), the IC 50 values were in the same concentration range as compared to adamantyl derivatives (0.19 to 1.1 µM) [88]. For heterocyclic derivatives, a pattern was noted: enlargement of the substituent lowered the IC 50 [88]. ...

... For the first time, the synergistic effect of compound 5 with the alkylating agent temozolomide was studied on glioblastoma lines. The leading compound is able to improve its cytostatic properties by up to 40% ( Figure 2) [13]. ...

... The analysis of these data suggests that in the both compounds the C=N bond of the isatin fragment has an E-configuration, and in the case of camphor the C=N bond of the monoterpene fragment in substance 6 has an E-configuration, and a Z-configuration in the case of fenchone in compound 7. We have previously shown that initial hydrazones 4 and 5 are in the form of a single isomer in a DMSO-d 6 or CHCl 3 solution [32]. An indirect proof of this mutual arrangement of the isatin and monoterpene fragments is the presence of cross peaks between H and 10-Me in the NOESY spectra (Fig. 1). ...