ICARST is fully involved it the research related to SARS-CoV-2 pandemy

18.11.2020

ICARST contributes through its join laboratories ICARST-Pharmaceutical Faculty, Commenius University, Bratislava and ICARST - University of SS. Cyril and Methodius, Trnava, to the APVV research project started on September 2020 entitled" New Antiviral Drugs: Design, Synthesis and Activity Evaluation of Specific Inhibitors of Viral Proteases of Coronavirus SARS-CoV-2" (PP-COVID-20-0010). Other partners in the research project are Faculty of Natural Sciences, CU, Bratislava, Institute of Chemistry and Institute of Virology, Slovak Academy of Sciences, Bratislava. Coordinating institution is University of SS. Cyril and Methodius Trnava.

The project strategy is based on an integrated approach and it is focused on: • Computer-assisted design and optimization of new specific peptidomimetic α-ketoamides that inhibit the proteolytic activity of Mpro and of a series of bis-benzylidene cyclohexanones that inhibit the deubiquitination activity of PLpro of the coronavirus SARS-CoV-2. • Development of synthetic routes and synthesis of peptidomimetic α-ketoamides and bisbenzylidenecyclohexanones. • Testing of inhibition of enzymatic activity of both groups of substances on recombinantly prepared enzymes Mpro and PLpro and development of new methods for testing for inhibitory activity on viral enzymes. • Testing the antiviral activity of both groups of substances at the level of inhibition of human cell lines infected with SARS-CoV-2 virus. • Research into the interactions of new inhibitors with biological membranes and optimization of absorption in the respiratory tract.

The results of first phase of the research have been published on November 4, 2020 in the recognized scientific journal of Royal Chemical Society, RSC Advances 2020, 10, 40244-40263 (https://pubs.rsc.org/is/content/articlepdf/2020/ra/d0ra08304f)