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

被引：89
|
作者：
Xie, ZF
Chai, KY
Piao, HR
Kwak, KC
Quan, ZS [1 ]
机构：
[1] Yanbian Univ, Coll Pharm, Yanji 133000, Jilin, Peoples R China
[2] Wonkwang Univ, Dept Chem, Iksan 570749, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 21期
基金：
中国国家自然科学基金;
关键词：
1,2,4]triazolo[4,3-a]quinolines; anticonvulsant; maximal electroshock; pentylenetetrazol; neurotoxicity;
D O I：
10.1016/j.bmcl.2005.07.051
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 (sc) 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 41 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. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4803 / 4805
页数：3
相关论文
共 50 条
  • [1] Synthesis and anticonvulsant activity of 7-benzylamino-4,5-dihydro-[1,2,4] triazolo[4,3-a] quinolines
    Cui Xiangshu1
    2.College of Basic Medicine
    3.College of Pharmacy
    Progress in Natural Science, 2007, (09) : 1104 - 1108
  • [2] Synthesis and anticonvulsant activity of 1-substituted-7-benzyloxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline
    Cui, LJ
    Xie, ZF
    Piao, HR
    Li, G
    Chai, KY
    Quan, ZS
    BIOLOGICAL & PHARMACEUTICAL BULLETIN, 2005, 28 (07) : 1216 - 1220
  • [3] Synthesis and anticonvulsant activity of 7-benzylamino-4, 5dihydro-[1,2,4] triazolo[4,3-a]quinolines
    Cui Xiangshu
    Guan Liping
    Li Hailan
    Piao Huri
    Quart Zheshan
    PROGRESS IN NATURAL SCIENCE-MATERIALS INTERNATIONAL, 2007, 17 (09) : 1104 - 1108
  • [4] Synthesis and anticonvulsant evaluation of 4-(4-alkoxylphenyl)-3-ethyl-4H-1,2,4-triazoles as open-chain analogues of 7-alkoxyl-4,5-dihydro[1,2,4]triazolo[4,3-a]quinolines
    Chen, Jing
    Sun, Xian-Yu
    Chai, Kyu-Yun
    Lee, Jin-Seok
    Song, Mi-Sun
    Quan, Zhe-Shan
    BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (21) : 6775 - 6781
  • [5] Synthesis of 2-substituted-7-heptyloxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-1(2H)-ones with anticonvulsant activity
    Wei, Cheng-Xi
    Li, Fu-Nan
    Zhao, Long-Xuan
    Zhao, Li-Ming
    Quan, Zhe-Shan
    ARCHIV DER PHARMAZIE, 2007, 340 (09) : 491 - 495
  • [6] Synthesis and Anticonvulsant Activity of 5-Phenyl-[1,2,4]-triazolo[4,3-a]quinolines
    Guan, Li-Ping
    Jin, Qing-Hao
    Wang, Shou-Feng
    Li, Fu-Nan
    Quan, Zhe-Shan
    ARCHIV DER PHARMAZIE, 2008, 341 (12) : 774 - 779
  • [7] Synthesis and Anticonvulsant Activities of 4-Alkoxyl-[1,2,4]Triazolo[4,3-a]Quinoxaline Derivatives
    Ren, Yang
    Shen, Qing-Kun
    Ding, Ming-Ming
    Yin, Xiu-Mei
    Quan, Zhen-Shan
    LATIN AMERICAN JOURNAL OF PHARMACY, 2016, 35 (10): : 2169 - 2175
  • [8] Anticonvulsant and toxicity evaluation of some 7-alkoxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline-1(2H)-ones
    Jin, Hong-Guang
    Sun, Xian-Yu
    Chai, Kyu-Yun
    Piao, Hu-Ri
    Quan, Zhe-Shan
    BIOORGANIC & MEDICINAL CHEMISTRY, 2006, 14 (20) : 6868 - 6873
  • [9] Synthesis and pharmacological activity of 1,2,4-triazolo[4,3-a]quinolines
    Savini, L
    Chiasserini, L
    Pellerano, C
    Filippelli, W
    Falcone, G
    FARMACO, 2001, 56 (12): : 939 - 945
  • [10] Synthesis and anticonvulsant activity study of 7-substituted phenoxyl-4,5-dihydro[1,2,4]triazolo[4,3-a]quinolines and quinoline-1(2H)-ones
    Jin, Yun-Zhe
    Guan, Li-Ping
    Zhao, Li-Ming
    Piao, Hu-Pi
    Quan, Zhe-Shan
    CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2007, 27 (12) : 1567 - 1572
12345