SYNTHESIS AND STRUCTURE OF 3-ARYLIDENE AND 3-HETARYLIDENE-1,2-DIHYDRO-3H-1,4-BENZODIAZEPIN-2-ONES AND THEIR AFFINITY TOWARD CNS BENZODIAZEPINE RECEPTORS

Authors

  • В. И. Павловский A. V. Bogatsky Physico-Chemical Institute, National Academy of Sciences of Ukraine, Division of Medicinal Chemistry, Odessa 65090
  • С. Ю. Бачинский A. V. Bogatsky Physico-Chemical Institute, National Academy of Sciences of Ukraine, Division of Medicinal Chemistry, Odessa 65090
  • Н. А. Ткачук A. V. Bogatsky Physico-Chemical Institute, National Academy of Sciences of Ukraine, Division of Medicinal Chemistry, Odessa 65090
  • С. Ю. Макан A. V. Bogatsky Physico-Chemical Institute, National Academy of Sciences of Ukraine, Division of Medicinal Chemistry, Odessa 65090
  • С. А. Андронати A. V. Bogatsky Physico-Chemical Institute, National Academy of Sciences of Ukraine, Division of Medicinal Chemistry, Odessa 65090
  • Ю. А. Симонов Institute of Applied Physics, Academy of Sciences of Moldova, Chisinau 2028
  • И. Г. Филиппова Institute of Applied Physics, Academy of Sciences of Moldova, Chisinau 2028
  • М. Гданец Chemical Faculty, A. Mickiewicz University, 60-780 Poznan

DOI:

https://doi.org/10.1007/7423

Keywords:

3-arylidene- and 3-hetarylidene-1, 2-dihydro-3H-1, 4-benzodiazepin-2-ones, affinity, central and peripheral benzodiazepine receptors

Abstract

The condensation of 5-aryl-7-bromo-1,2-dihydro-3H-1,4-benzodiazepin-2-ones with aromatic aldehydes gives 5-aryl-3-arylidene- and 5-aryl-7-bromo-3-hetarylidene-1,2-dihydro–3H-1,4–benzodiazepin–2–ones. X-ray diffraction structural analysis yielded the  molecular and crystal structures of 7-bromo-3-(4'-
methoxybenzylidene)-5-phenyl-1,2-dihydro-3H-1,4-diazepin-2-one and showed that this compound has cis configuration. Radioligand analysis was used to  study the affinity of these products toward central nervous system and peripheral benzodiazepine receptors.

How to Cite
Pavlovsky, V. I.; Bachinskii, S. Yu.; Tkachuk, N. A.; Makan, S. Yu.; Andronati, S. A.; Simonov, Yu. A.; Filippova, I. G.; Gdaniec, M.  Chem. Heterocycl. Compd. 2007, 43, 1029. [Khim. Geterotsikl. Soedin. 2007, 1213.]

For this article in the English edition see DOI 10.1007/s10593-007-0161-3


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Published

2023-02-02

Issue

No. 8 (2007)

Section

Original Papers