Archiv der Pharmazie

, volume 346 , issue 2 , pages 119-126

Synthesis and Anticonvulsant Activity Evaluation of 5-Phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amines

Yan Zheng ¹

Ming Bian ^{1, 2}

Xian-Qing Deng ¹

Shi-Ben Wang ¹

Zheshan Quan ¹

Hide authors affiliations Show authors affiliations: 2 affiliations

College of Pharmacy, Yanbian University,Yanji City, Jilin, China |

Institute of Pharmaceutical Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Inner Mongolia Autonomous Region, Tongliao, China |

Publication type: Journal Article

Publication date: 2012-12-18

Wiley

Archiv der Pharmazie

scimago Q2

wos Q2

SJR: 0.571

CiteScore: 7.0

Impact factor: 3.6

ISSN: 03656233, 15214184

DOI: 10.1002/ardp.201200376

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PubMed ID: 23255333

Drug Discovery

Pharmaceutical Science

Abstract

In the present study we describe the syntheses and anticonvulsant activity evaluation of 5-phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amine derivatives. Their anticonvulsant activity and neurotoxicity were evaluated by the maximal electroshock seizure test (MES) and the rotarod test, respectively. The majority of the compounds prepared were effective in the MES screens at a dose level of 100 mg/kg. Of these compounds, the most promising was compound 8h, which showed an ED50 value of 27.4 mg/kg and a protective index (PI) value of 5.8. These values were superior to those provided by valproate (ED50 and PI values of 272 and 1.6, respectively) in the MES test in mice. As well as its anti-MES efficacy, the potencies of compound 8h against seizures induced by pentylenetetrazole and thiosemicarbazide were also established, with the results suggesting that the GABAergic system-mediated mechanisms might be involved in its anticonvulsant activity.

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Zheng Y. et al. Synthesis and Anticonvulsant Activity Evaluation of 5-Phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amines // Archiv der Pharmazie. 2012. Vol. 346. No. 2. pp. 119-126.

GOST all authors (up to 50) Copy

Zheng Y., Bian M., Deng X., Wang S., Quan Z. Synthesis and Anticonvulsant Activity Evaluation of 5-Phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amines // Archiv der Pharmazie. 2012. Vol. 346. No. 2. pp. 119-126.

RIS |

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RIS Copy

TY - JOUR

DO - 10.1002/ardp.201200376

UR - https://doi.org/10.1002/ardp.201200376

TI - Synthesis and Anticonvulsant Activity Evaluation of 5-Phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amines

T2 - Archiv der Pharmazie

AU - Zheng, Yan

AU - Bian, Ming

AU - Deng, Xian-Qing

AU - Wang, Shi-Ben

AU - Quan, Zheshan

PY - 2012

DA - 2012/12/18

PB - Wiley

SP - 119-126

IS - 2

VL - 346

PMID - 23255333

SN - 0365-6233

SN - 1521-4184

ER -

BibTex |

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BibTex (up to 50 authors) Copy

@article{2012_Zheng,

author = {Yan Zheng and Ming Bian and Xian-Qing Deng and Shi-Ben Wang and Zheshan Quan},

title = {Synthesis and Anticonvulsant Activity Evaluation of 5-Phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amines},

journal = {Archiv der Pharmazie},

year = {2012},

volume = {346},

publisher = {Wiley},

month = {dec},

url = {https://doi.org/10.1002/ardp.201200376},

number = {2},

pages = {119--126},

doi = {10.1002/ardp.201200376}

}

MLA

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MLA Copy

Zheng, Yan, et al. “Synthesis and Anticonvulsant Activity Evaluation of 5-Phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amines.” Archiv der Pharmazie, vol. 346, no. 2, Dec. 2012, pp. 119-126. https://doi.org/10.1002/ardp.201200376.

Publisher

Wiley

Journal

Archiv der Pharmazie

scimago Q2

wos Q2

SJR

0.571

CiteScore

7.0

Impact factor

3.6

ISSN

03656233 (Print)

15214184 (Electronic)