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Information × Registration Number 0220U103636, 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 29-10-2020 Organization Physico-Chemical Institute O. Bogatsky National Academy of Sciences of Ukraine popup.description2  The purpose of the study: Study of the peculiarities of reactions of 1,4-benzodiazepine with carbonyl compounds. Establishing the structure of substances formed by their chemical properties, affinity for BDR and pharmacological properties, the relationship between structure and properties. Synthesis of new types of "asymmetric" 3-arylidene-5-[(E)-2-(aryl)vinyl]-1,2-dihydro-3H-1,4-benzdiazepin-2-ones. Synthesis of new 3-substituted 1,3-dihydro-2H-1,4-benzdiazepin-2-ones containing piperazinebenzoic acid fragments. To determine the anticonvulsant effect of compound 007 in a model of corazol-induced kindling in mice, and to evaluate the characteristics of the dynamics of redistribution by seizures of varying severity. To study the analgesic effect of compound 007 in the conditions of combined (somatogenous and neuropathic) pain syndrome in diabetic neuropathy. The method of synthesis of 1,4-benzdiazepin-2-ones was used to obtain the previously described series of 5-[(E)-2-(4-phenylvinyl)]-1,2-dihydro-3H-1,4-benzdiazepin-2-one. Condensation of aldehydes, for example benzophenone, adamantanone and fluarenone, with 7-bromo-5-phenyl-1,3-dihydro-2H-1,4-benzdiazepin-2-one was carried out. It is shown that the best yields of condensation products at position "3" of the 1,4-benzdiazepine cycle are obtained using cesium carbonate as a base. The use of sodium or potassium carbonates reduces the yields and contamination of the target products. The affinity of the synthesized 3-arylidene-1,2-dihydro-3H-benzdiazepin-2-ones to benzodiazepine receptors was established by radioligand analysis. It is shown that the new 3-arylidene-5-phenyl-1,3-dihydro-2H-1,4-benzdiazepin-2-ones show analgesic activity with ED50 values from 0.08 to 0.88 mg/kg. The effectiveness and safety of long-term analgesic action of the innovative compound 007 has been proven, which is necessary to create a dossier for the drug and for further registration of the compound of regulatory bodies of Ukraine according Product Description popup.authors Andronati Sergei A Bachinsky Sergey Yu. Burenkova Natalia O. Duma Hanna І. Kabanova Tetyana A. Karaseva Tamara L. Karpenko Olexander S. Kornylov Olexander Yu. Krysko Andrii А. Lyakhov Sergey A Soboleva Svetlana H. Нalimova Olena I. Shibinskaya Marina O. popup.nrat_date 2021-03-17 Close