Synthesis and anticonvulsant activity of novel purine derivatives

Wang, Shi‐Ben; Jin, Peng; Li, Fu-Nan; Quan, Zhe‐Shan

doi:10.1016/j.ejmech.2014.07.074

Cited by 21 publications

(19 citation statements)

References 26 publications

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“…Compounds 14a was the most potent compound, with an ED 50 of 23.4 mg/kg and a PI value of more than 25.6 after intraperitoneal administration in mice. Furthermore, it showed significant oral activity in MES test in mice, with an ED 50 of 39.4 mg/kg and a PI above 31.6 46 .…”

Section: -Substituted-124-triazolesmentioning

confidence: 96%

“…Several [1,2,4]triazolo[4,3-g]purines ( 113 , Figure 17 ) were also prepared by Quan’s group to more effective AEDs. Compounds 113a and 113b were considered as the most promising compounds with an ED 50 of 51.2 and 51.9 mg/kg in MES test, respectively 46 . Meanwhile, a series of triazolopyrimidines were prepared and evaluated for their anticonvulsant activities.…”

Section: Fused-triazolesmentioning

confidence: 99%

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Recent developments on triazole nucleus in anticonvulsant compounds: a review

Song

Deng

2018

Journal of Enzyme Inhibition and Medicinal Chemistry

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Epilepsy is one of the common diseases seriously threatening life and health of human. More than 50 million people are suffering from this condition and anticonvulsant agents are the main treatment. However, side effects and intolerance, and a lack of efficacy limit the application of the current anticonvulsant agents. The search for new anticonvulsant agents with higher efficacy and lower toxicity continues to be the focus and task in medicinal chemistry. Numbers of triazole derivatives as clinical drugs or candidates have been frequently employed for the treatment of various types of diseases, which have proved the importance of this heterocyclic nucleus in drug design and discovery. Recently many endeavours were made to involve the triazole into the anticonvulsants design, which have brought lots of active compounds. This work is an attempt to systematically review the research of triazole derivatives in the design and development of anticonvulsant agents during the past two decades.

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Section: -Substituted-124-triazolesmentioning

confidence: 96%

Section: Fused-triazolesmentioning

confidence: 99%

Recent developments on triazole nucleus in anticonvulsant compounds: a review

Song

Deng

2018

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…The SAR studies revealed that the replacement of triazole ring with other heterocycles such as imidazole, methylimidazole, and pyrazole results in compounds with decreased activity and higher neurotoxicity. Moreover, when the triazolyl moiety was replaced by 1,2,4-triazol-3-ylthio group, the obtained compounds showed no activity [49].…”

Section: N-aryltriazolesmentioning

confidence: 97%

The importance of triazole scaffold in the development of anticonvulsant agents

Ayati

Emami

Foroumadi

2016

European Journal of Medicinal Chemistry

107

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Epilepsy is one of the most important neurological disorders with high prevalence worldwide. Many epileptic patients are not completely treated with available drugs and need multiple therapies. Also, many antiepileptic drugs have shown unwanted side effects and drug interactions. Therefore there are continuing interests to find new anticonvulsant drugs. Triazole ring has been found in the structure of many compounds with diverse biological effects. Due to the success of several triazole-containing drugs that entered the pharmaceutical market as CNS-active drugs, this class of heterocyclic compounds has great importance for discovery and development of new anticonvulsant drugs. In this article, we have tried to summarize the latest efforts which have been made in the design and development of triazole-derived anticonvulsant agents.

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“…Among the compounds studied, compound 217 was the most potent compound, with a ED 50 of 23.4 mg/kg and a high protective index of more than 25.6 after intraperitoneal administration in mice (Figure 12). Compound 217 showed significant oral activity against MES-induced seizures in mice, with an ED 50 of 39.4 mg/kg and a PI above 31.6 [169].…”

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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Synthesis and anticonvulsant activity of novel purine derivatives

Cited by 21 publications

References 26 publications

Recent developments on triazole nucleus in anticonvulsant compounds: a review

Recent developments on triazole nucleus in anticonvulsant compounds: a review

The importance of triazole scaffold in the development of anticonvulsant agents

Current Research on Antiepileptic Compounds

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