Literature DB >> 16139502

Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines.

Zhi-Feng Xie1, Kyu-Yun Chai, Hu-Ri Piao, Kyung-Chell Kwak, Zhe-Shan Quan.   

Abstract

A series of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline derivatives was synthesized using 6-hydroxy-3,4-dihydro-1H-quinolin-2-one as a starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES test) and the subcutaneous (s.c.) pentylenetetrazol test (scMet test), and their neurotoxicity was evaluated by the rotarod neurotoxicity test (Tox). MES and scMet tests show that 7-(4-fluorobenzyloxy)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline 4l was found to be the most potent with ED50 value of 11.8 and 6.7 mg kg(-1) and protective index (PI = TD50/ED50) value of 4.6 and 8.1, respectively.

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Year:  2005        PMID: 16139502     DOI: 10.1016/j.bmcl.2005.07.051

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  A ligand-based computational drug repurposing pipeline using KNIME and Programmatic Data Access: case studies for rare diseases and COVID-19.

Authors:  Alzbeta Tuerkova; Barbara Zdrazil
Journal:  J Cheminform       Date:  2020-11-25       Impact factor: 5.514

2.  A ligand-based computational drug repurposing pipeline using KNIME and Programmatic Data Access: case studies for rare diseases and COVID-19.

Authors:  Alzbeta Tuerkova; Barbara Zdrazil
Journal:  J Cheminform       Date:  2020-11-25       Impact factor: 5.514

3.  Synthesis of Novel 7-Substituted-5-phenyl-[1,2,4]triazolo[1,5-a] Pyrimidines with Anticonvulsant Activity.

Authors:  Nan Jiang; Xian-Qing Deng; Fu-Nan Li; Zhe-Shan Quan
Journal:  Iran J Pharm Res       Date:  2012       Impact factor: 1.696

4.  Synthesis and Anticonvulsant Activity Evaluation of 3-alkoxy-4-(4-(hexyloxy/heptyloxy)phenyl)-4H-1,2,4 -triazole.

Authors:  Ying-Quan Fang; Chun-Ling Sun; Da-Chuan Liu; Shi-Ben Wang; Zhe-San Quan
Journal:  Iran J Pharm Res       Date:  2015       Impact factor: 1.696

5.  Efficient Synthesis and in Silico Studies of the Benzimidazole Hybrid Scaffold with the Quinolinyloxadiazole Skeleton with Potential α-Glucosidase Inhibitory, Anticoagulant, and Antiplatelet Activities for Type-II Diabetes Mellitus Management and Treating Thrombotic Disorders.

Authors:  S Shashidhar Bharadwaj; Boja Poojary; Sharath Kumar M Nandish; Jayanna Kengaiah; Mugaranja P Kirana; Madan Kumar Shankar; Anupam J Das; Ananda Kulal; Devaraja Sannaningaiah
Journal:  ACS Omega       Date:  2018-10-03

Review 6.  Recent developments on triazole nucleus in anticonvulsant compounds: a review.

Authors:  Ming-Xia Song; Xian-Qing Deng
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

  6 in total

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