In sti tute of mo lec u lar bi ol ogy and ge net ics NAS of Ukraine Academicain Zabolotnog str., 150, Kyiv, 03680 Ukraine shved_@ imbg.org. ua De sign and syn the sis of a set of 3,5-dioxy-1,2,4-triazinyl-6-propionic acid (TPA) arylamides were de veloped in or der to search for new com pounds with fungistatic prop er ties on the ba sis of azapyrimidine de riv atives. Carboxamides ca pa ble to block tran scrip tion were re vealed among ob tained com pounds us ing T7 RNA-pol model test-sys tem in vi tro, and the only de riv a tives con tain ing halogene-substituent in pharmacophore part showed the in hib i tory prop er ties. The model of vir tual tri ple non-pro duc tive com plex at poly mer ase cat a lytic site (in hib i tor-en zyme-DNA tem plate) was pro posed, il lus trat ing a pos si ble mech anism of in hib i tory ac tion of such com pounds on RNA syn the sis. Pre lim i nary screen ing of new triazine de riva tives re vealed their in hib i tory ac tion against some kinds of fungi and bac te ria.Keywords: 1,2,4-triazine de riv a tives, syn the sis, sup pres sion of tran scrip tion, T7 RNA-pol, antifungal ac tivity.
441ISSN 0233-7657. Biopolymers and cell. 2007. vol. 23. N 5. Translated from Ukrainian.
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