Synthesis of Novel 8-alkylamino-5, 6-dihydro-4H-benzo[f] [1,2,4]triazolo [4,3-a]azepines as Anticonvulsant Agents

Wu, Hui-Fan; Han, Rong-bi; Jin, Chun-Zi; Piao, Fengyuan

doi:10.2174/1871527315666160321111211

Cited by 3 publications

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“…As a continuation of the previous work, a series of new 8-alkylamino-5,6-dihydro-4 H -benzo[f][1,2,4]triazolo [4,3-a]azepine derivatives were synthesised and screened for their anticonvulsant activities by the MES test, scPTZ test, and rotarod test. The results of these tests showed that 8-heptylamino-5,6-dihydro-4 H -benzo[f][1,2,4]triazolo[4,3-a]azepine ( 136 , Figure 22 ) was the most promising compound, with an ED 50 of 19.0 mg/kg, and PI value of 14.8 in the MES test, which is much higher than the PI value of the prototype antiepileptic drug carbamazepine (PI = 8.1), phenytoin (PI = 6.9), phenobarbital (PI = 3.2), and sodium valproate (PI = 1.6) 151 .…”

Section: Fused-triazolesmentioning

confidence: 96%

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: Fused-triazolesmentioning

confidence: 96%

Recent developments on triazole nucleus in anticonvulsant compounds: a review

Song

Deng

2018

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…10 ) by using the principle of electron equivalence, replacing sulfur atom of compound 36 with carbon atom. All the compounds were tested in the convulsant model including MES and PTZ, and the safety of some of them was higher than that of the control drugs carbamazepine and sodium valproate 56 . It also provides a reference for the design of compounds in the future.…”

Section: Polycyclic Triazolementioning

confidence: 99%

An Important Potential Anti-Epileptic/Anticonvulsant Active Group: A Review of 1,2,4-Triazole Groups and Their Action

Wang

Liu

2021

Drug Res (Stuttg)

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Epilepsy is one of the most common encountered neurological disorders. Many individuals continue to have seizures despite medical and surgical treatments, suggesting new antiepileptic/anticonvulsant drugs are required. Triazole compounds are widely used in pharmaceuticals and have gained significant importance in medicinal chemistry. This article is an attempt to systematically review the research of triazole derivatives in the design and development of anticonvulsant agents during the past two decades through extensive literature research. The results show that triazole occupy a distinct niche in heterocyclic chemistry and represent a key motif in medicinal chemistry because of their capability to exhibit an array of properties and bioactivities, Therefore, 1,2,4-triazole seems to be an important pharmacophore, especially in the field of antiepileptic, which is of great explored potentiality and utilized value. Through in-depth research on this type of structure, it is believed that more 1,2,4-triazole compounds will be developed as anti-epileptic drugs for clinical use.

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An Active Group with Potential Anti-seizure Activity: A Review on 1,2,4- Triazoles

Wang

Quan

Liu

2023

LDDD

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Background: Epilepsy is one of the most common neurological disorders. Many individuals continue to have seizures despite medical and surgical treatments, suggesting that the discovery of novel antiseizure drugs is vital. Triazole compounds are widely used as pharmaceuticals and have gained significant interest in medicinal chemistry. In this article, the development of triazoles, especially 1,2,4-triazole, in the field of antiseizure therapeutics is reviewed. Method: The relevant literature was investigated, classified, and analysed. This article attempts to systematically review the research of triazole derivatives in the design and development of antiseizure agents during the past two decades through extensive literature research, which was based on the information accessible in PubMed, Science Direct, Google Scholar and other databases. Results: Research results demonstrate that triazoles occupy a distinct niche in heterocyclic chemistry and represent a key motif in medicinal chemistry because of their ability to exhibit an array of properties and bioactivities. Therefore, 1,2,4-triazole appears to be an important pharmacophore, especially in the field of antiseizure therapeutics, where its promising potential value has been explored. Conclusion: This review presents a summary of the research related to 1,2,4-triazole which acts as a potential antiseizure pharmacophore that could be further developed. Compounds with 1,2,4-triazole or related structures had previously shown reasonable antiseizure activity and safety. After thorough research of this structure, it is believed that 1,2,4-triazole-containing compounds will be further developed as antiseizure drugs for clinical use.

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Synthesis of Novel 8-alkylamino-5, 6-dihydro-4H-benzo[f] [1,2,4]triazolo [4,3-a]azepines as Anticonvulsant Agents

Cited by 3 publications

References 0 publications

Recent developments on triazole nucleus in anticonvulsant compounds: a review

Recent developments on triazole nucleus in anticonvulsant compounds: a review

An Important Potential Anti-Epileptic/Anticonvulsant Active Group: A Review of 1,2,4-Triazole Groups and Their Action

An Active Group with Potential Anti-seizure Activity: A Review on 1,2,4- Triazoles

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