Design, synthesis, and evaluation of anticonvulsant activities of benzoxazole derivatives containing the 1,2,4‐triazolone moiety

2019 ◽  
Vol 352 (8) ◽  
pp. 1800313 ◽  
Author(s):  
Ming‐Xia Song ◽  
Yuping Huang ◽  
Shiben Wang ◽  
Zeng‐Tao Wang ◽  
Xian‐Qing Deng
Keyword(s):  
Design Synthesis ◽  
Anticonvulsant Activities

scholarly journals Design, Synthesis, Characterisation & Anticonvulsant Activities of Novel Heterocyclic Substituted Isatin Derivatives

2020 ◽  
Vol 11 (4) ◽  
pp. 6351-6362
Author(s):  
Kosaraju Lahari ◽  
Raja Sundararajan
Keyword(s):  
Pharmacophore Model ◽  
Epileptic Activity ◽  
Anticonvulsant Drugs ◽  
Rotarod Test ◽  
Design Synthesis ◽  
Active Analog ◽  
Chemical Structures ◽  
Anticonvulsant Activities ◽  
Isoxazole Derivatives ◽  
Isatin Derivatives

Twelve new isoxazole/pyrazole/pyrimidine substituted 5-nitrosation analogues were designed according to the requirements of the anticonvulsant drugs pharmacophore model and synthesised from indole-2,3-dione. Entire prepared compounds chemical structures were established from its IR, proton-NMR, Mass spectrum & microanalysis data. Anticonvulsant potency of final isatin analogues was assessed by MES technique & sc PTZ technique. Besides rotarod test was used to assess the neurotoxicity of all potent title analogues. Title compounds exhibited a varying degree of anticonvulsant potency ranging from mild to good. In the present study, it was concluded that pyrazole derivatives exhibited higher anti-epileptic activity than isoxazole derivatives. However, pyrimidine analogues displayed inferior activity than isoxazole analogues. 4-(2-(4-(1-((Dimethylamino)methyl)-5-nitro-2-oxindole-3-ylideneamino)phenyl) hydrazone)-1-(4-chlorophenyl)-3-amino-1H-pyrazole-5(4H)-one 7c was established as the most active analog of this series. Hence this derivative can act as a pilot molecule for further progress of new effective anticonvulsant drugs.

Design, Synthesis, and Characterization of High-Affinity, Systemically-Active Galanin Analogues with Potent Anticonvulsant Activities

2008 ◽  
Vol 51 (24) ◽  
pp. 8038-8047 ◽  
Author(s):  
Grzegorz Bulaj ◽  
Brad R. Green ◽  
Hee-Kyoung Lee ◽  
Charles R. Robertson ◽  
Karen White ◽  
...  
Keyword(s):  
Synthesis And Characterization ◽  
Design Synthesis ◽  
High Affinity ◽  
Anticonvulsant Activities

Design, Synthesis and Evaluation of the Antidepressant and Anticonvulsant Activities of Triazole-Containing Benzo[d]oxazoles

2017 ◽  
Vol 16 (2) ◽  
pp. 187-198 ◽  
Author(s):  
Ming-Xia Song ◽  
Bao-Qi Rao ◽  
Bin-Bin Cheng ◽  
Bentham Science Publisher Yi ◽  
Bentham Science Publisher Wu ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Anticonvulsant Activities

Design, synthesis, preliminary pharmacological evaluation, and docking studies of pyrazoline derivatives

2012 ◽  
Vol 66 (1) ◽  
Author(s):  
Nirupam Das ◽  
Biswajit Dash ◽  
Meenakshi Dhanawat ◽  
Sushant Shrivastava
Keyword(s):  
Chemical Structure ◽  
Motor Coordination ◽  
Docking Studies ◽  
Monoamine Oxidase A ◽  
Good Activity ◽  
Activity Profile ◽  
Design Synthesis ◽  
Rota Rod Test ◽  
Anticonvulsant Activities ◽  
Derivatives Of

AbstractTen derivatives of N1 substituted/unsubstituted 5-(4-chlorophenyl)-3-(2-thienyl) pyrazoline were synthesised from chalcone-like intermediate and substituted phenyl hydrazines, hydrazine hydrate, and semi/thiosemicarbazide. The chemical structure of compounds was confirmed by means of IR, 1H NMR, mass spectroscopy, and elemental analysis. The antidepressant and anticonvulsant activities were investigated by Porsolt’s behavioural despair test (forced swimming) and maximum electroshock seizure test, respectively. Rota-Rod test was performed to assess any probable changes in motor coordination induced by the test compounds. Four compounds (IId, IIg, IIi, and IIj) exhibited good activity profile against depression and docking studies confirmed their consensual interaction with monoamine oxidase A. In addition, compounds IIc and IIe showed protection against MES-induced seizures.

Sign in / Sign up

Export Citation Format

Share Document