Search academic texts

Information × Registration Number 0221U101183, 0120U104785 , R & D reports Title Polypharmacophoric organic compounds based on peptidomimetics and annelated benzodiazepines popup.stage_title Head Chebanov Valentyn A., Доктор хімічних наук Registration Date 16-01-2021 Organization State Scientific Institution Scientific and Technological Complex" Institute of Single Crystals "of the National Academy of Sciences of Ukraine popup.description2  At the first stage of the project, the following main tasks were solved: analysis of literature data; development of new and improvement of existing methods for the synthesis of reagents and intermediates; the study of the physicochemical properties of the synthesized compounds, spectral and chromatographic studies; creation of a pharmacophore models for certain targets, the impact on which is associated with the antimicrobial activity; studу of the solubility of the synthesized compounds in accordance with the requirements of the State Pharmacopoeia of Ukraine. As a result of the work, the analysis of literature data on the tandem combination of multicomponent and click-reactions was carried out. A method for the preparation of pyrolone derivatives with a free carboxyl group is proposed. Synthetic routes have been developed for the preparation of 4-aryl-5-aminoimidazole derivatives containing functional groups that can participate in the Ugi reaction. An efficient and environmentally friendly procedure for producing 2-azidobenzaldehyde has been developed. Selective methods for the synthesis of N-(2-amino-1-(2-azidophenyl)-2-oxoethyl) propiolamides have been developed. A reagent for the synthesis of extended peptidomimetics is obtained - 2 (1- (tert-butyl) -1H-tetrazol-5-yl) propan-2-amine. Pharmacophore models of NLRP3 and TLR7 receptors were constructed, which, based on the results of validation, demonstrated their high predictive ability to recognize active and inactive agonists of these receptors. The solubility of five synthesized substances in 14 solvents has been proved and evaluated. Detailed information on the purity, molecular structure, and physicochemical properties of the synthesized compounds was obtained. Product Description popup.authors popup.nrat_date 2021-01-16 Close