Volume 20 No 10 (2022)
 Download PDF
SYNTHESIS AND PHARMACOLOGICAL SCREENING OF 2-AZETIDINONE DERIVATIVES: AS A NOVEL ANTICONVULSANT AGENT
S.P. Kumbhar , S.S. Patil
Abstract
A new series of 2-Azetidinone derivative 3a-3f were prepared by reacting 4-(furan-2-yl)-6-methyl-2-oxo1,2,3,4-tetrahydropyrimidine-5-carbo hydrazide with aromatic aldehyde then cyclization was done along with chloroacetyl chloride in presence of triethyl amine and 1, 4-dioxane. They were screened for anticonvulsant activity by Isoniazid (INH) and Pentylenetetrazole (PTZ) induced convulsions in mice. The structures of the derivatives were elucidated by FT-IR, 1H NMR, 13C NMR and HRMS.All the compounds were given satisfactory reaction yields that represented the efficiency of the employed synthetic route. INH induced convulsion model, delayed the onset of convulsion significantly3b, 3c, 3d, 3eanf 3f when compared to an induction control group. Whereas delayed onset of convulsion was non-significant for 3a. In PTZ induced convulsion model, delayed the onset of convulsion significantly 3c and 3f when compared to the induction control group. Whereas delayed onset of convulsion was non-significant for 3a, 3b, 3d and 3e.This indicates the anticonvulsant activity of these derivatives which might be due toenhancement of GABA mediated inhibitory activity. This anticonvulsant activity was due to the presence of electron withdrawing groups like Br, CF3 and electron donating groups like NH2, CH3, OH at the 2 nd and 4th position of the aromatic ring attached to 2-Azetidinone moiety.
Keywords
2-Azetidinone, convulsion, Isoniazid, PTZ, GABA
Copyright
Copyright © Neuroquantology

Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Articles published in the Neuroquantology are available under Creative Commons Attribution Non-Commercial No Derivatives Licence (CC BY-NC-ND 4.0). Authors retain copyright in their work and grant IJECSE right of first publication under CC BY-NC-ND 4.0. Users have the right to read, download, copy, distribute, print, search, or link to the full texts of articles in this journal, and to use them for any other lawful purpose.