Search academic texts

Information × Registration Number 0219U000882, 0117U003444 , R & D reports Title Synthesis, molecular, crystalline structure and properties of ligands of benzodiazepine and fibrinogen receptors. popup.stage_title Head Andronati S.A., Registration Date 12-03-2019 Organization A.V. Bogatsky, Physico-Chemical Institute of the National Academy of Sciences of Ukraine popup.description2 A series of new ligands of low-affinity forms of fibrinogen receptors, derivatives of 2-piperazinyl-3,4-dihydro-quinazolin-4-one, containing residues of (1R,3S)-3-aminocyclopentanecarboxylic acid, 3-aminocyclohexanecarboxylic acid and cis-4- aminocyclohexanecarboxylic acids was obtained. The molecular and crystalline structure of tetrahydrate of 6-(4-piperazinium-4-yl-benzoylamino)-2-(piperazine-1-yium)-4-oxo-3,4-dihydroquinazolin-1-yl chloride sulfate was established by PCA. It has been found that the compounds inhibit platelet aggregation in vivo with IC50 values from 17 ?M to 0.02 ?M. It was showed that studied quinazolin-4-ones inhibited the binding of fibrinogen to alfaIIbbetta3 with IC50 values to from 9 ?M to 0.04 ?M. A series of new 3-arylidene-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepine-2-ones were synthesized, their structures were confirmed by mass spectrometry and 1H-NMR spectroscopy. The affinity of synthesized 3-arylidene(hetarylidene)-1,2-dihydro-3H-benzodiazepine-2-ones for benzodiazepine receptors was determined by the method of radio-ligand analysis. Product Description popup.authors А.А. Крисько О. М. Дехтяренко О.І. Халімова О.Ю. Корнілов С.А. Андронаті С.С. Декіна С.Ю. Бачинський Т.А. Кабанова popup.nrat_date 2020-04-02 Close