SCHIFF BASES OF 2,4-DIHYDROXYBENZALDEHYDE AS POTENTIAL ANTICONVULSANT COMPOUNDS; IN VIVO AND DOCKING STUDIES

被引:0
作者
Murtaza, Shahzad [1 ]
Akhtar, Muhammad Shoaib [2 ]
Aslam, Ayesha [2 ]
Riaz, Tauqeer [1 ]
Kousar, Naghmana [1 ]
机构
[1] Univ Gujrat, Fac Sci, Dept Chem, Gujrat 50700, Pakistan
[2] Univ Sargodha, Dept Pharmacol, Fac Pharm, Sargodha, Pakistan
来源
ACTA POLONIAE PHARMACEUTICA | 2017年 / 74卷 / 06期
关键词
epilepsy; in vivo studies; docking studies; carbonic anhydrases; GABA level; sedative effect; ROOT EXTRACT; PATHOPHYSIOLOGY;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The present study was aimed to evaluate the anticonvulsant activity of 2,4-dihydroxybenzaldehyde derivatives. The experimental group of mice have been subjected to pentylenetetrazole. strychnine and picrotoxin induced convulsions. Different convulsion parameters including onset of convulsion, duration of convulsion, number of animal convulsed and percentage protection were studied. A constant dose dependent increase in onset and reduction in duration of convulsions was observed along with significant protection from death in different groups of mice. The tested compounds showed comparable anticonvulsant activity to that of standard drug phenytoin. Four compounds showed highly significant anticonvulsant effect in case of picrotoxin-induced convulsions while the other two compounds gave significant results against the convulsions. The molecular docking studies were performed with carbonic anhydrases and the binding interaction values reinforced the experimental results. The effect of tested compounds on brain GABA level was also estimated by spectrophotometric method. Compounds 1 at lower dose (150 mg/kg) were found to significantly (p < 0.001) increase the brain GABA level. The tested compounds also showed sedative effect by potentiating the sleeping time with diazepam in different groups of mice.
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收藏
页码:1717 / 1728
页数:12
相关论文
共 32 条
  • [1] Anticonvulsant, anxiolytic and sedative activities of the aqueous root extract of Securidaca longepedunculata Fresen.
    Adeyemi, O. O.
    Akindele, A. J.
    Yemitan, O. K.
    Aigbe, F. R.
    Fagbo, F. I.
    [J]. JOURNAL OF ETHNOPHARMACOLOGY, 2010, 130 (02) : 191 - 195
  • [2] Synthesis and anticonvulsant activity of some newer dihydro-pyrimidine-5-carbonitrile derivatives: Part II
    Ali, Mohammad R.
    Verma, Garima
    Shaquiquzzaman, Mohammad
    Akhter, Mymoona
    Alam, Mohammad M.
    [J]. JOURNAL OF TAIBAH UNIVERSITY MEDICAL SCIENCES, 2015, 10 (04): : 437 - 443
  • [3] Synthesis and biological evaluation of some 4-(6-substituted-1,3-benzothiazol-2-yl)amino-1, 3-thiazole-2-amines and their Schiff bases
    Amnerkar, Nikhil D.
    Bhongade, Bhoomendra A.
    Bhusari, Kishore P.
    [J]. ARABIAN JOURNAL OF CHEMISTRY, 2015, 8 (04) : 545 - 552
  • [4] [Anonymous], ASIAN J BIOMED PHARM
  • [5] Asif M., 2013, Iran. J. Pharm. Sci, V9, P67
  • [6] The Protein Data Bank
    Berman, HM
    Westbrook, J
    Feng, Z
    Gilliland, G
    Bhat, TN
    Weissig, H
    Shindyalov, IN
    Bourne, PE
    [J]. NUCLEIC ACIDS RESEARCH, 2000, 28 (01) : 235 - 242
  • [7] Anticonvulsant activity of Mimosa pudica decoction
    Bum, EN
    Dawack, DL
    Schmutz, M
    Rakotonirina, A
    Rakotonirina, SV
    Portet, C
    Jeker, A
    Olpe, HR
    Herding, P
    [J]. FITOTERAPIA, 2004, 75 (3-4) : 309 - 314
  • [8] Dichter MA, 2009, ARCH NEUROL-CHICAGO, V66, P443, DOI 10.1001/archneurol.2009.10
  • [9] Dunbrack R. L., 2009, CURR OPIN STRUC BIOL, V12, P431
  • [10] Engelborghs S, 2000, ACTA NEUROL BELG, V100, P201