Search academic texts

Information × Registration Number 0220U103588, 0115U002146 , R & D reports Title Ligands of benzodiazepine, serotonin, dopamine, and fibrinogen receptors. Synthesis, "structure-property" relationship, selectivity and bi(poly)modality of action popup.stage_title Head Andronati Sergey A., Доктор хімічних наук Registration Date 23-10-2020 Organization Physico-Chemical Institute O. Bogatsky National Academy of Sciences of Ukraine popup.description2 Purpose of the work: Synthesis and study of the properties of potential antiplatelet agents based on 2-piperazin-1-yl-3H-quinazolin-4-one derivatives. New derivatives quinazolin-4-one derivatives containing p-aminomethylbenzoic, p-piperidinbenzoic, L-3-amino-2-ethoxycarbonylaminopropionic, L-3-amino-2-isobutoxycarbonylaminopropionic, L-3-amino-2-benzoxycarbonyl-aminopropionic or L-4-amino-2-benzoxycarbonylaminobutanoic acids were synthesized. Molecular docking of quinazolin-4-one derivatives to the fibrinogen receptor model was carried out. Final derivatives of quinazolin-4-one showed high antiaggregatory activity in vitro experiments on a platelet-rich human blood plasma, with IC50 values ranging from 1.9*10-6 to 1.0*10-8 M. The effect of quinazolin-4-one derivatives on the specific binding of a fluorescein-labeled fibrinogen (FITC-Fg) to its receptors on a slurry of washed human platelets. The best indicator of IC50 belongs compound containing in its composition the residue of L-4-amino-2-benzoxycarbonylaminobutanoic acid and equals 1.53*10-9 M.  Product Description popup.authors Illyushko Natalia О. Bachinsky Serhii Yu. Kabanova Tetyana A. Karaseva Tamara L. Kornylov Аlexander Yu. Krysko Andrii А. Krysko Olga L. Pavlovskyi Viktor I. Нalimova Olena I. popup.nrat_date 2021-03-17 Close