Structure and properties of 1,4-benzodiazepine and related heterocyclic systems derivatives
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ANDRONATI, Sergei, SIMONOV, Yurii A., PAVLOVSKY, Victor, MAKAN, Svetlana, KARASEVA, T.. Structure and properties of 1,4-benzodiazepine and related heterocyclic systems derivatives. In: Physical Methods in Coordination and Supramolecular Chemistry, 27 septembrie - 1 octombrie 2006, Chişinău. Chisinau, Republic of Moldova: 2006, XVII, p. 37. ISBN 978-9975-62-066-6.
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Physical Methods in Coordination and Supramolecular Chemistry
XVII, 2006
Conferința "The XV-th International Conference Physical Methods in Coordination and Supramolecular Chemistry : The XVII-th Reading in memory of Acad. A.Ablov"
Chişinău, Moldova, 27 septembrie - 1 octombrie 2006

Structure and properties of 1,4-benzodiazepine and related heterocyclic systems derivatives


Pag. 37-37

Andronati Sergei1, Simonov Yurii A.2, Pavlovsky Victor1, Makan Svetlana3, Karaseva T.3
 
1 A.V. Bogatsky Physical-Chemical Institute of NASU,
2 Institute of Applied Physics,
3 A.V. Bogatsky Physico-Chemical Institute of the NAS of Ukraine
 
Disponibil în IBN: 4 iunie 2020


Rezumat

Derivatives of 1,4-benzodiazepine and related heterocyclic condensed heterosystems containing nitrogen have important pharmacological properties. Psychotropic properties provoked by influence of this compounds on GABAА receptors functioning are the most interesting. It has been established that α-subunits (benzodiazepine receptors, BDR), which are included in the content of GABAА receptors, are molecular targets of benzodiazepines. The kind and level of BDR ligands activity, selectivity of ligand-receptor interaction are determined by both ligand structure and subtype as well as BDR isoform. The elucidation of structural and conformational peculiarities of BDR ligands is a necessary stage at the studying of «structure – properties» relationships of GABA-ergic psychotropic agents. Compounds I-VIII were synthesized at the studying of structure function relations of potential BDR ligands.figureStructure of substances has been established by the methods of IR, UV spectroscopy, X-ray analysis, mass-spectrometry and NMR spectroscopy. The character of intermolecular relationships of compounds and inclusive complexes formed by them has been studied. Influence of substituent of R1 nature on the rate and thermodynamic parameters of inversion of dihydro-1,4-benzodiazepines I (n=2) hetero ring has been demonstrated through the method of dynamic 1Н and 19F NMR. The presence of two non equivalent conformations (pseudoboat and form with anticlinal conformation of amide group) of dihydrobenzodiazepinones (I n = 2) has been found. It has been shown that the most active anticonvulsants of I type (n=2) are prevalent in the pseudoboat conformation. High affinity for BDR and high activity have been found for the series of representatives of compounds I-VIII through the several psychopharmacological tests. Influence of both electronic and steric factors on the ligand recognition by benzodiazepine receptor and their pharmacological properties has been found.