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Information × Registration Number 0221U100577, 0119U002807 , R & D reports Title Synthesis and antiaggregative activity of fibrinogen receptor antagonists based on 2,6-diaminoquinazolines scaffold that containing residue of -substituted GABA. popup.stage_title Head Kornylov Oleksandr Yu., Registration Date 07-01-2021 Organization Physico-Chemical Institute O. Bogatsky National Academy of Sciences of Ukraine popup.description2 The research objects – derivatives of 2,6-diaminoquinazolines containing piperazin-1-yl, homopiperazin-1-yl and 2,5-diazabicyclo[2.2.1]hept-2-yl in the second position of the quinazoline heterocycle; and the amides of 3-substituted GABAs - in the sixth position of the quinazoline heterocycle. The aim of 2nd stage of research – synthesis of the main building-blocks based on 2-piperazinylquinazoline and homological structures comprising homopiperazin-1-yl and 2,5-diazabicyclo[2.2.1]hept-2-yl; synthesis of target “non-classical” fibrinogen receptor antagonists based on 2,6-diaminoquinazolines; biological evaluation of antiaggregation activity and affinity for αIIbβ3; analysis of the relationship between structure, activity and affinity. Synthesis of a series of “non-classical” fibrinogen receptor antagonists based on derivatives of 2,6-diaminoquinazolines containing amides of 3-substituted GABAs in their structures was carried out. The structure and purity of the compounds synthesized were confirmed by NMR-spectroscopy, MS-spectrometry and by HPLC. In vitro platelet aggregation assays have demonstrated ranging of activity from IC50 = 0.27 mМ to IC50 = 2.2 mМ. It was found that the introduction of homoperiperazine into the 2nd position of quinazoline heterocycle and the use of 3-(4-chlorophenyl)-GABA as substituent at the 6th position have a negative influence on the activity. In a series of the compounds synthesized, leading structures have been established. The experimental data of study provides the framework for a further research in the creation of potent safe antiplatelet agents promising for use in medicine.   Product Description popup.authors Kornylov Olexander Yu. popup.nrat_date 2021-03-17 Close