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Registration Number

0220U103650, 0115U002146 , R & D reports

Title

Ligands of benzodiazepine, serotonin, dopamine, and fibrinogen receptors. Synthesis, "structure-property" relationship, selectivity and bi(poly)modality of action

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Head

Andronati Sergey A., Доктор хімічних наук

Registration Date

29-10-2020

Organization

Physico-Chemical Institute O. Bogatsky National Academy of Sciences of Ukraine

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 The purpose of the study: Synthesis of new ligands of benzodiazepine, serotonin, CNS receptors and fibrinogen receptor antagonists: to establish the structural-coformational factors that determine the selectivity of ligand-receptor interactions and pharmacological properties, as well as bi- or polymodal action of ligands. A synthesis method has been developed and a number of new 2-aminochalcones have been obtained, conditions have been selected for the preparation of 5-styryl-1,2-dihydro-1,4-benzodiazepines on their basis. The synthesis of new 3-phthalimidoacyl-1,4-benzodiazepin-2-ones has been carried out. Condensation of 3-chloro-1,4-benzodiazepin-2-ones with o-, m-, p-fluoro, or o-, m-, p-chloroanilines synthesized a series of 3-chlorophenyl- and 3-(fluorophenyl)amino-1,4-benzodiazepin-2-ones. A synthesis method was proposed for obtaining the previously described series of 5-[(E)-2-(4-phenylvinyl)]-1,2-dihydro-3H-1,4-benzodiazepin-2-ones. Condensation of benzophenone, adamantanone or fluarenone with 7-bromo-5-phenyl-1,4-benzodiazepin-2-one has been carried out. It is shown that the best yields of the target products are obtained when using cesium carbonate as a base. Optically active 3-alkyl-5-[(E) -2 (aryl)vinyl]-1,2-dihydro-3H-1,4-benzodiazepin-2-ones have been synthesized. A number of new 1,4-benzdiazepin-2-ones containing piperazine benzoic acid residues at position 3 have been synthesized. Using the immobilized microsomal fraction, enantioselective hydrolysis of 3-acetoxy-7-bromo-5-phenyl-1,4-benzodiazepin-2-one was carried out and the S-enantiomer of the substrate was obtained. The affinity of 3-phthalimidoacyl 1,4-benzodiazepin-2-ones to the BDR of the central nervous system was studied and it was found that compounds of this series have a high affinity. When studying the effect of 1,4-benzodiazepine derivatives on the appetite of rats using the "Anorexia" method, it was shown that some compounds exhibit anorexigenic effect.

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Andronati Sergey A.
Bachinsky Sergey Yu.
Burenkova Natalia O.
Golovenko Mykola Ya
Dekina Svetlana S.
Duma Hanna І.
Kabanova Tetyana A.
Karpenko Olexander S.
Kornylov Olexander Yu.
Krysko Andrii А.
Larionov Vitaliy B.
Lyakhov Sergey A
Ryzhak Аlexandra А.
Romanovska Irina I.
Soboleva Svetlana H.
Нalimova Olena I.
Tsapenko Zhanna М.
Shesterenko Yevgeniia А.
Shibinskaya Marina O.

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2020-10-29