Design, synthesis and anticonvulsant activities of novel 1-(substituted/unsubstituted benzylidene)-4-(4-(6,8-dibromo-2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl)phenyl) semicarbazide derivatives

2012 ◽  
Vol 22 (9) ◽  
pp. 3072-3078 ◽  
Author(s):  
Govindaraj Saravanan ◽  
Veerachamy Alagarsamy ◽  
Chinnasamy Rajaram Prakash
Keyword(s):  
Design Synthesis ◽  
Anticonvulsant Activities ◽  
Methyl Phenyl

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.

scholarly journals Design, Synthesis, and Acaricidal Activity of Phenyl Methoxyacrylates Containing 2-Alkenylthiopyrimidine

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3379
Author(s):  
Shulin Hao ◽  
Zengfei Cai ◽  
Yangyang Cao ◽  
Xiaohua Du
Keyword(s):  
Mass Spectra ◽  
Field Trials ◽  
Acaricidal Activity ◽  
Tetranychus Cinnabarinus ◽  
Ovicidal Activity ◽  
Design Synthesis ◽  
Rapid Action ◽  
Ld50 Value ◽  
Greenhouse Tests ◽  
Methyl Phenyl

A series of novel phenyl methoxyacrylate derivatives containing a 2-alkenylthiopyrimidine substructure were designed, synthesized, and evaluated in terms of acaricidal activity. The structures of the title compounds were identified by 1H NMR, 13C NMR and high-resolution mass spectra (HRMS). Compound (E)-methyl 2-(2-((2-(3,3-dichloroallylthio)-6-(trifluoromethyl)pyrimidin-4-yloxy)methyl)phenyl)-3-methoxyacr-ylate (4j) exhibited significant acaricidal activity against Tetranychus cinnabarinus (T. cinnabarinus) in greenhouse tests possessing nearly twice the larvicidal and ovicidal activity compared to fluacrypyrim. Furthermore, the results of the field trials demonstrated that compound 4j could effectively control Panonychuscitri with long-lasting persistence and rapid action. The toxicology data in terms of LD50 value confirmed that compound 4j has a relatively low acute toxicity to mammals, birds, and honeybees.

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

scholarly journals Design, Synthesis and Fungicidal Activity of Novel (E)-Methyl 2-{2-[(coumarin-7-yloxy)methyl]phenyl}-3-methoxyacrylates

2007 ◽  
Vol 2 (8) ◽  
pp. 1934578X0700200
Author(s):  
Chang-Ling Liu ◽  
Miao Li ◽  
Ai-Ying Guan ◽  
Hong Zhang ◽  
Zheng-Ming Li
Keyword(s):  
Downy Mildew ◽  
Fungicidal Activity ◽  
Biological Activities ◽  
Design Synthesis ◽  
Cucumber Downy Mildew ◽  
Coumarin 7 ◽  
Methyl Phenyl

A number of 7-hydroxycoumarins (5), on treatment with one equivalent of ( E)-methyl 2-{2-[(chloromethyl)phenyl]}-3-methoxyacrylate (6) at 80°C for 6–8 h, afforded ( E)-methyl 2-{2-[(coumarin-7-yloxy)methyl]phenyl}-3-methoxyacrylates (2) in 80–85% yields. The 7-hydroxycoumarins (5) were in turn prepared from resorcinols (3) and substituted ethyl 3-oxopropanoate (4). Subsequently, results of biological activities evaluated in the greenhouse indicated that several of these compounds have good fungicidal activity against cucumber downy mildew (CDM) at 25g ai/ha.

scholarly journals Anticonvulsant Activities of 4-benzylidene-6-(4-methyl-phenyl)-4,5-dihydropyridazin-(2H)-ones and 4-benzylidene-6-(4-chloro-phenyl)-4,5-dihydropyridazin-(2H)-ones

2016 ◽  
Vol 3 (1) ◽  
pp. 203-214 ◽  
Author(s):  
Mohammad Asif ◽  
Anita Singh
Keyword(s):  
Maximum Activity ◽  
Anticonvulsant Agents ◽  
Phenytoin Sodium ◽  
Methyl Derivatives ◽  
Chloro Derivatives ◽  
Anticonvulsant Activities ◽  
Dose Levels ◽  
Near Future ◽  
Methyl Phenyl

Background: Two series of 4-benzylidene-6-(4-methyl-phenyl)-4,5-dihydropyridazin-(2H)-one compounds (3a-e) and 4-benzylidene-6-(4-chloro-phenyl)-4,5-dihydropyridazin-(2H)-ones (3f-j) were synthesized and evaluated as anticonvulsant agents. Methods: Synthesized compounds (3a-3j) were tested against maximum electro shock (MES) and Isoniazid (INH) induced convulsion methods for anticonvulsant activities and neurotoxicity. Results: In MES induced convulsions, result found that the compounds 3e and 3j exhibited highest anticonvulsant activities. In INH induced convulsions, result was indicated that all the compounds exhibited good anticonvulsant activities., whereas compounds 3d and 3j showed maximum activity. Methyl derivatives were more active than chloro derivatives. Phenytoin sodium (25mg/kg) and sodium vaproate (50mg/kg) were used as reference drugs. All these synthesized pyridazinone compounds (3a-j) did not exhibit any neurotoxicity up to 100 mg/kg dose levels. Conclusion: All compounds showed good anticonvulsant activities against both MES and INH induced convulsion models. Many such explorations are anticipated in the near future.

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