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Information × Registration Number 0209U005450, 0107U008554 , R & D reports Title Directional search for synthetic antibacterial compounds against specific human infections. popup.stage_title Head Tukalo Mykhaylo, Доктор біологічних наук Registration Date 17-02-2009 Organization Institute of molecular biology & genetics popup.description2 As a result of a work on the project a number of compounds inhibiting prolyl-tRNA synthetase from Enterococcus faecalis, one of the most dangerous Gram-positive pathogen, were found. This was achieved with modified virtual screening technique that was implemented for 100,000 organic compounds collection. On the base of calculation results 150 promising compounds were selected. Using three independent methods for in vitro assay the effect of the 150 compounds on enzymatic activities of E. faecalis and S. pneumonie prolyl-tRNA synthetases were tested. Three compounds, quinoline derivatives (named compounds № 58, 138 and 150) have shown most significant effect of inhibition for both prolyl-tRNA synthetases in the range IC50 from 30 to 90 ?M, were selected. Result obtained is one of the most important for the Project's aim, because it allowed to discover "starting" biological activity which became the base for further chemical optimization of active compounds and the synthesis and testing of novel compounds with higher activity and with better physical and chemical properties. Product Description popup.authors popup.nrat_date 2020-04-02 Close