- Synthesis, spectroscopic characterization, X-ray structure, and in vivo neurotropic activity of new 1,5-benzodiazepin-2-ones
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The paper reports the synthesis and in vivo pharmacological studies of a series of N-alkyl-1,5-benzodiazepine-2-ones. In this work, 19 novel benzodiazepine derivatives have been prepared and characterized by spectroscopic methods including 2D nuclear magnetic resonance techniques. Crystal structure of 1-benzyl-8-methyl-4-phenyl-1H-benzo[b][1,4]diazepin-2(3H)-one has also been determined by X-ray diffraction. Prediction of activity spectra for substances prediction and docking studies onto human serum albumin were conducted. Two compounds under these investigation showed high antihypoxic, tranquilizing, and anticonvulsant activity in vivo.
- Gaponov, Alexandr A.,Zlenko, Elena T.,Shishkina, Svetlana V.,Shishkin, Oleg V.,Antypenko, Oleksii M.,Tretiakov, Serhii V.,Palchikov, Vitaliy A.
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p. 1768 - 1780
(2016/10/03)
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- Enantioselective synthesis of 4-substituted 4,5-dihydro-1 H-[1,5]benzodiazepin-2(3 H)-ones by the Lewis base-catalyzed hydrosilylation
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Enantioselective synthesis of 4-substituted 4,5-dihydro-1H-[1,5] benzodiazepin-2(3H)-ones has been accomplished through chiral Lewis base-catalyzed hydrosilylation. The corresponding products were obtained in excellent yields (up to 99%) and enantioselect
- Chen, Xing,Zheng, Yongsheng,Shu, Chang,Yuan, Weicheng,Liu, Bo,Zhang, Xiaomei
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experimental part
p. 9109 - 9115
(2011/12/16)
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- Polycyclic α-amino-ε-caprolactams and related compounds
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Disclosed are polycyclic α-amino-ε-caprolactams and related compounds which are useful as synthetic intermediates in the preparation of inhibitors of β-amyloid peptide release and/or its synthesis.
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Page/Page column 56
(2010/02/14)
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- Substituted-2,3-dihydro-2-oxo-1,5-benzodiazepines and their use as fungicides
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A method of controlling fungi comprising contacting the fungi with a fungicidally effective amount of a benzodiazepine of the structure: wherein, R1 is substituted or unsubstituted, straight or branched alkyl having from 3 to 10 carbon atoms, or substitut
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- SYNTHESIS AND MASS SPECTRA OF 2,3-DIHYDRO-1H-1,5-BENZODIAZEPINE-2-THIONES
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2,3-Dihydro-1H-1,5-benzodiazepine-2-thiones and their N-methyl and S-methyl derivatives were synthesized.It was demonstrated by means of the IR, UV, PMR, and mass spectra that in solutions with different polarities 1,5-benzodiazepine-2-thiones exist prima
- Solomko, Z. F.,Sharbatyan, P. A.,Gaponov, A. A.,Avramenko, V. I.
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p. 341 - 345
(2007/10/02)
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- Action de l'hydroxylamine sur les dihydro-1,3 benzodiazepine-1,5 thiones (ones)-2
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The reaction of hydroxylamine with 4-phenyl-1,5-benzodiazepin 2-thiones(ones) 1-6 has been investigated.Depending upon the starting benzodiazepine either the 3-phenyl-5-N-(2-amino phenyl)amino isoxazoles 8, 10, 11 3-N-(2-aminophenylimino) 3-phenyl propionohydroxamic acid or 3-phenyl 5-isoxazolone 14 was obtained.The structure of compounds 8, 10, 11 have been unambiguously established by catalytic hydrogenation.A mechanism for this transposition has been suggested.
- Essassi, El Mokhtar,Salem, Moussa,Viallefont, Philippe
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p. 890 - 892
(2007/10/02)
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