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Information × Registration Number 0216U000772, 0114U004607 , R & D reports Title Synthesis, properties, molecular and crystal structure of ligands of the benzodiazepine and fibrinogen receptors popup.stage_title Head Andronati S.A., Registration Date 25-02-2016 Organization A.V.Bogatsky Physico-Chemical Institute of the National Academy of Sciences of Ukraine popup.description2 Research object: derivatives of 1,2,3,4-tetrahydroisoquinoline phtalimidine and 1,4-benzodiazepine-2-ones. Objective: Synthesis, the establishment of structural features and conformational properties of potential ligands of benzodiazepine and fibrinogen receptor, the study of relationship "structure - properties - molecular mechanism of action." There were synthesized novel fibrinogen receptor antagonists, derivatives of 1,2,3,4-tetrahydroisoquinoline, quinazoline and phtalimidine. Synthesized compounds exhibit antiaggregating activity (ІC50 from 10-6 to 10-8 mol/L) and affinity for the fibrinogen receptor (ІC50 from 10-6 to 10-9 mol/L). Among the 3-arylamino-1,4-benzodiazepine-2-ones the series of selective ligands PBDR - 3-(nitrophenyl)amino-1,2-dihydro-3H-1,4-benzodiazepine-2-ones were found 1-metoxycarbonylmethyl-3-(nitrophenyl)amino-1,2-dihydro-3H-1,4-benzodiazepine-2-one hose demonstrated a highest affinity Ki = 19,1 ± 3,0 nm.5481 Product Description popup.authors А.А. Крисько В.І. Павловський Г.В. Самойленко О.Л. Крисько О.М. Дехтяренко Т.А. Кабанова Т.Л. Карасьова Т.О. Юрпалова Я.Р. Кривенко popup.nrat_date 2020-04-02 Close