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Synthesis and Anticonvulsant Activity of Various Mannich and Schiff Bases of 1,5-Benzodiazepines
Joint Authors
Pandeya, Surendra N.
Rajput, Neha
Source
International Journal of Medicinal Chemistry
Issue
Vol. 2012, Issue 2012 (31 Dec. 2012), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2012-11-28
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
Benzodiazepines have a various behavioral effects in addition to their anxiolytic action.
There is every reason to believe that the BZ/GABA receptor complex is involved in these effects, since GABAmimetic manipulations modify the effect of BZ in tests of convulsive activity, motor function, and appetitive behavior.
1,5-Benzodiazepines are biologically important molecules and are extensively used clinically as analgesic, hypnotic, sedative, and antidepressive agents.
Hence, 1,5-Benzodiazepines were synthesized by condensation of o-phenylenediamine and ketones, for example, cyclohexanone and acetone in presence of sulfated zirconia (catalyst).
Mannich bases were synthesized with acetophenone, p-nitroacetophenone, p-chloroacetophenone, and formaldehyde.
Schiff bases were synthesized using Mannich base of 1,5-benzodiazepines with p-chloroaniline and p-chlorophenylsemicarbazide in the presence of glacial acetic acid.
All the synthesized compounds were characterized by 1H NMR and IR spectral analyses.
All the synthesized derivatives were evaluated at the dose of 30 mg/kg b.w for anticonvulsant activity by isoniazid induced convulsion model, and the compounds NBZD-3 and NBZD-8 were found to be the most active among all compounds.
Among all the synthesized derivatives, compounds NBZD-13 and NBZD-17 were found to be the most active among all compounds using thiosemicarbazide induced model.
Although NBZD-8, NBZD-10, and NBZD-18 are the compounds which had shown good anticonvulsant activity and have an advantage over that, they were not sedative.
American Psychological Association (APA)
Pandeya, Surendra N.& Rajput, Neha. 2012. Synthesis and Anticonvulsant Activity of Various Mannich and Schiff Bases of 1,5-Benzodiazepines. International Journal of Medicinal Chemistry،Vol. 2012, no. 2012, pp.1-10.
https://search.emarefa.net/detail/BIM-456293
Modern Language Association (MLA)
Pandeya, Surendra N.& Rajput, Neha. Synthesis and Anticonvulsant Activity of Various Mannich and Schiff Bases of 1,5-Benzodiazepines. International Journal of Medicinal Chemistry No. 2012 (2012), pp.1-10.
https://search.emarefa.net/detail/BIM-456293
American Medical Association (AMA)
Pandeya, Surendra N.& Rajput, Neha. Synthesis and Anticonvulsant Activity of Various Mannich and Schiff Bases of 1,5-Benzodiazepines. International Journal of Medicinal Chemistry. 2012. Vol. 2012, no. 2012, pp.1-10.
https://search.emarefa.net/detail/BIM-456293
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-456293