SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME SCHIFF BASES OF [4-(AMINO)-5-PHENYL-4H-1, 2, 4-TRIAZOLE-3-THIOL]

被引:0
作者
Jubie, Selvaraj [1 ]
Sikdar, Pranabesh [1 ]
Antony, Shanish [2 ]
Kalirajan, Rajagopal [1 ]
Gowramma, Byran [1 ]
Gomathy, Subramanian [1 ]
Elango, Kannan [1 ]
机构
[1] JSS Coll Pharm, Dept Pharmaceut Chem, Rocklands, Ooty, India
[2] JSS Coll Pharm, Dept Pharmacol, Rocklands, Ooty, India
关键词
Triazole; Schiff bases; antianxiety; antidepressant;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The basic nucleus 4-(amino)-5-phenyl-1-4H-1,2,4-triazole-3-thiol was prepared by cyclisation of potassium dithiocarbazinate with hydrazine hydrate using water as solvent under reflux condition for 3-4 h. The compound which has been synthesized successfully was subjected to addition reaction with different aldehydes to synthesize Schiff bases. The compounds were confirmed by physical parameters (solubility, melting point), chromatographic methods (TLC) and at last spectroscopic methods (IR, NMR, and Mass). In order to ascertain the pharmaceutical application, the selective pharmacological screening of the derivatives was carried out according to the standard procedures. The compounds were screened for their antianxietic activity by elevated plus maze method, antidepressant activity by forced swim test. Among the synthesized compounds, the Schiff bases of benzaldehyde (5e), furfuraldehyde (5d) and 2,4-dichloro benzaldehyde (5a) showed extremely significant activities. Results indicate that these compounds may be potential candidates for managing CNS disorders. However further studies are required to substantiate the same which are underway in our lab.
引用
收藏
页码:109 / 112
页数:4
相关论文
共 7 条
  • [1] Synthesis, antibacterial and antifungal activity of 4-substituted-5-aryl-1,2,4-triazoles
    Colanceska-Ragenovic, K
    Dimova, V
    Kakurinov, V
    Molnar, DG
    Buzarovska, A
    [J]. MOLECULES, 2001, 6 (10) : 815 - 824
  • [2] Synthesis characterization and anticancer activity studies on some Mannich bases derived from 1,2,4-triazoles
    Holla, BS
    Veerendra, B
    Shivananda, MK
    Poojary, B
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2003, 38 (7-8) : 759 - 767
  • [3] Studies on synthesis and pharmacological activities of 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and their dihydro analogues
    Mathew, Vinod
    Keshavayya, J.
    Vaidya, V. P.
    Giles, D.
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2007, 42 (06) : 823 - 840
  • [4] Synthesis and biological activity of new derivatives of 3-(3,4-diaryl-1,2,4-triazole-5-yl)propenoic acid
    Modzelewska-Banachiewicz, B
    Banachiewicz, J
    Chodkowska, A
    Jagiello-Wójtowicz, E
    Mazur, L
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2004, 39 (10) : 873 - 877
  • [5] Sharma R., 2008, IND DRUGS, V45, P859
  • [6] Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential HIV-1NNRTIs
    Wu, Jingde
    Liu, Xinyong
    Cheng, Xianchao
    Cao, Yuan
    Wang, Defeng
    Li, Zhong
    Xu, Wenfang
    Pannecouque, Christophe
    Witvrouw, Myriam
    De Clercq, Erik
    [J]. MOLECULES, 2007, 12 (08) : 2003 - 2016
  • [7] ZANGROSSI H, 2004, PHARM RES, V50, P517