Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine

Guan, Liping; Sui, Xin; Deng, Xian‐Qing; Quan, Ying-Chun; Quan, Zhe‐Shan

doi:10.1016/j.ejmech.2009.12.077

Cited by 46 publications

(20 citation statements)

References 24 publications

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“…In initial screening and quantitative evaluation, compound 194 was the most active agent, exhibiting the lowest toxicity at the same time (Table 10). In the anti-MES test, it showed ED50 of 17.3 mg/kg and TD50 of 380.3 mg/kg, and the PI of 22.0 which is much better than PI of the reference drugs [156].…”

Section: The Pyridazine Functional Groupmentioning

confidence: 99%

Current Research on Antiepileptic Compounds

2015

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Epilepsy affects about 1% of the world's population. Due to the fact all antiepileptic drugs (AEDs) have some undesirable side effects and about 30% of epileptic patients are not seizure-free with the existing AEDs, there is still an urgent need for the development of more effective and safer AEDs. Based on our research work on antiepileptic compounds and other references in recent years, this review covers the reported work on antiepileptic compounds which are classified according to their structures. This review summarized 244 significant anticonvulsant compounds which are classified by functional groups according to the animal model data, although there are some limitations in the data. This review highlights the properties of new compounds endowed with promising antiepileptic properties, which may be proven to be more effective and selective, and possibly free of unwanted side effects. The reviewed compounds represent an interesting possibility to overcome refractory seizures and to reduce the percentage of patients with a poor response to drug therapy.

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Section: The Pyridazine Functional Groupmentioning

confidence: 99%

Current Research on Antiepileptic Compounds

2015

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“…Pyrazolopyridazines derivatives were being reported for biological and pharmacological activities such as antimicrobial , anti‐inflammatory , and inhibitors of GSK‐3 . Pyridazine and pyrimidine derivatives have been previously reported to be platelet‐aggregation inhibitors, α‐adrenoceptor antagonists, antihypertensive, antinociceptive, antimicrobial, and antiparkinsonism . Heterocyclic nitrogen compounds are responsible for the mechanism of the drug activity, for example, in Zidovudine (Retrovir) .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Reactions, and Pharmacological Evaluations of Some Novel Pyridazolopyridiazine Candidates

Fayed

Al-Harbi

Amr

et al. 2014

Journal of Heterocyclic Chem

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OCH 3Herein, we report the synthesis, characterization, and preliminary pharmacological activity of a new series of substituted pyrazolopyridazine derivatives. Compound 1 was reacted with ethoxymethylene malononitrile 2 in refluxing ethanol to give the corresponding compound 3, which was treated with hydrazine hydrate or formamide to give pyrazolo[3,4-c]pyrazole 4 and pyrazolo pyrimidine 5 derivatives, respectively. Also, compound 3 was reacted with NH 4 SCN or carbon disulphide or ethyl acetoacetate to yield the corresponding pyrazolo derivatives 6-8, respectively. Additionally, compound 3 was reacted with triethyl orthoformat in acetic anhydride to give 9, which was treated with hydrazine hydrate to give hydrazino derivative 10. The latter compound transformed into the pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]-pyrimidine 11 via refluxing with acetic anhydride. Finally, compound 9 was reacted with benzoic acid hydrazide or mercapto acetic acid to give compounds 12 and 13, respectively. The latter compound was treated with refluxing ethanolic sodium ethoxide solution to afford the pyrazolothiazolopyrimidine 14. Some of the compounds exhibited better activities as anti-inflammatory and antimicrobial agents than the reference controls. The detailed synthesis, spectroscopic data, anti-inflammatory, and antimicrobial activities of the synthesized compounds was reported.

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“…[1524][1525][1526][1527][1528] Article can be accessed online on: www.ijpsr.com Considerable interest has been attracted towards the pyridazine-3-one scaffold and its derivatives due to their widespread applications such as anticonvulsant activity 1 , antimicrobial activity 2 , antiviral activity 3 , anticancer 4 and analgesic activity 5 .…”

Section: Quick Response Code Doimentioning

confidence: 99%

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2013

IJPSR

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Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine

Cited by 46 publications

References 24 publications

Current Research on Antiepileptic Compounds

Current Research on Antiepileptic Compounds

Synthesis, Reactions, and Pharmacological Evaluations of Some Novel Pyridazolopyridiazine Candidates

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