Anticonvulsant and sedative-hypnotic activity of some novel 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2yl]-2-styrylquinazoline-4(3H)-ones

被引:0
|
作者
Sushil K. Kashaw
Vivek Gupta
Varsha Kashaw
P. Mishra
J. P. Stables
N. K. Jain
机构
[1] Dr. H.S. Gour University,Pharmaceutical Chemistry Division, Department of Pharmaceutical Sciences
[2] National Institutes of Health,Preclinical Pharmacology Section, Epilepsy Branch
来源
关键词
4(3; )-quinazolinones; MES; Subcutaneous pentylenetetrazole-induced seizure; CNS depressant activity;
D O I
暂无
中图分类号
学科分类号
摘要
A few novel 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones were synthesized and evaluated for anticonvulsant, neurotoxicity, sedative-hypnotic, and phenobarbitone-induced hypnosis potentiation test. After i.p. injection to mice at doses of 30, 100, and 300 mg/kg body weight derivatives were examined in the maximal electroshock-induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models in mice. Spectroscopic data were consistence with the newly synthesized compounds. The neurotoxicity was assessed using the Rotorod method. Out of 15 compounds only 7e and 7o showed anticonvulsant activity at various doses in one or more test models. All except 7d, 7m, and 7n exhibited significant sedative-hypnotic activity via actophotometer screen. Central nervous system (CNS)-depressant activity screened with the help of the forced swim method resulted into some potent compounds. No percentage increase in the sleeping time was observed in any of the synthesized compounds evaluated by the phenobarbitone-induced hypnosis potentiation test. On the basis of experimental data, it can be concluded that synthesized compounds possessed relatively better sedative-hypnotic and CNS-depressant activities.
引用
收藏
页码:250 / 261
页数:11
相关论文
共 50 条
  • [31] 5-[(4,6-Dimethylpyrimidin-2-ylsulfanyl)-methyl]-3-(morpholinomethyl)-1,3,4-oxadiazole-2(3H)-thione
    Thiruvalluvar, A.
    Subramanyam, M.
    Lingappa, B.
    Kalluraya, Balakrishna
    ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2007, 63 : O3425 - U2700
  • [32] 5-(3,4,5-Trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
    Saeed, Aamer
    Akram, Muhammad
    Rauf, Abdul
    Bolte, Michael
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2010, 66 : O1911 - U280
  • [33] ZnII and CuII complexes generated from 5-(pyridin-4-yl)-3-[2-(pyridin-4-yl)ethyl]-1,3,4-oxadiazole-2(3H)-thione
    Zhao, Hang-Ju
    Ma, Jian-Ping
    Liu, Qi-Kui
    Dong, Yu-Bin
    ACTA CRYSTALLOGRAPHICA SECTION C-STRUCTURAL CHEMISTRY, 2013, 69 : 716 - +
  • [34] Synthesis of 3-[3-(4′-methyl-benzenesulfonamido)phenyl]-5-(4-substituted phenyl)-1-acetyl-2-pyrazolines
    Havaldar, FH
    Khatri, NK
    ASIAN JOURNAL OF CHEMISTRY, 2005, 17 (02) : 1337 - 1339
  • [35] Spiro-heterocycles containing 1,3,4-oxadiazole: A convenient synthesis of 3-(5-substituted phenyl-1,3,4-oxadiazole-2-yl)-5,8-dithiaspiro[3,4]-octan-2-ones and 1,4-dithia-6-azaspiro[4,4]-nonan-7-ones
    Tiwari, Shailendra
    Singh, Kamal Pratap
    Pathak, Poonam
    Ahmad, Akeel
    INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY, 2018, 57 (08): : 1060 - 1064
  • [36] 5-(4,4"-Difluoro-5′-hydroxy-1,1′:3′,1"-terphenyl-4′-yl)-3-(morpholin-4-yl-methyl)-1,3,4-oxadiazole-2(3H)-thione
    Fun, Hoong-Kun
    Arshad, Suhana
    Samshuddin, S.
    Narayana, B.
    Sarojini, B. K.
    ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2011, 67 : O3372 - U192
  • [37] Antimicrobial activity of novel 3-substituted-5-(pyridine-4-yl)-3H-1,3,4-oxadiazole-2-thione derivatives
    Oza, K. K.
    Patel, H. S.
    BULGARIAN CHEMICAL COMMUNICATIONS, 2010, 42 (02): : 103 - 106
  • [38] Synthesis and anticonvulsant activity of some (2/4-substituted)benzaldehyde (2-oxobenzothiazolin-3-yl)acetohydrazones
    Çakir, B
    Yildirim, E
    Ercanli, T
    Erol, K
    Sahin, MF
    FARMACO, 1999, 54 (11-12): : 842 - 845
  • [39] Crystal structure of 3-{[4-(2-methoxyphenyl)piperazin-1-yl] methyl}-5-(thiophen-2-yl)-1,3,4-oxadiazole-2(3H)-thione
    Al-Alshaikh, Monirah A.
    Abuelizz, Hatem A.
    El-Emam, Ali A.
    Abdelbaky, Mohammed S. M.
    Garcia-Granda, Santiago
    ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2016, 72 : 269 - +
  • [40] Synthesis of new 3-(3-phenyl-isoxazol-5-yl) or 3-[(3-phenyl-isoxazol-5-yl)-amino] substituted 4(3H)-quinazolinone derivatives with antineoplastic activity
    Raffa, D
    Daidone, G
    Schillaci, D
    Maggio, B
    Plescia, F
    PHARMAZIE, 1999, 54 (04): : 251 - 254