Literature DB >> 19674817

Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea.

Sushil K Kashaw1, Varsha Kashaw, Pradeep Mishra, N K Jain, J P Stables.   

Abstract

Several new 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea were synthesized and screened for anticonvulsant, CNS depressant and sedative-hypnotic activity in the mice. After i.p. injection to mice at doses of 30, 100, and 300 mg/kg body weight synthesized compounds were examined in the maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. Spectroscopic data and elemental analysis were consistent with the newly synthesized compounds. The neurotoxicity was assessed using the rotorod method. Compounds E1, E6, E9, E12, P3, P4 and P6 were found to be active in the MES screen whereas E1, P4, P6 and P11 were found to be active in the scPTZ screen. All except E6, E11 and P6 showed more than 50% decrease in locomotor activity at 1h of compound administration via actophotometer screen. CNS depressant activity screened with the help of the forced swim method resulted into some potent compounds. All the compounds were found to exhibit potent CNS depressants activity as indicated by increased immobility time. It can be concluded that newly synthesized compounds possessed promising CNS activities.

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Year:  2009        PMID: 19674817     DOI: 10.1016/j.ejmech.2009.05.008

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  11 in total

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5.  Synthesis and analgesic activity of some new pyrazoles and triazoles bearing a 6,8-dibromo-2-methylquinazoline moiety.

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6.  Molecular Docking and Anticonvulsant Activity of Newly Synthesized Quinazoline Derivatives.

Authors:  Hatem A Abuelizz; Rabab El Dib; Mohamed Marzouk; El-Hassane Anouar; Yousreya A Maklad; Hanan N Attia; Rashad Al-Salahi
Journal:  Molecules       Date:  2017-06-30       Impact factor: 4.411

7.  Synthesis, in vitro antitumour activity, and molecular docking study of novel 2-substituted mercapto-3-(3,4,5-trimethoxybenzyl)-4(3H)-quinazolinone analogues.

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Review 8.  Primaquine derivatives: Modifications of the terminal amino group.

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Journal:  Eur J Med Chem       Date:  2019-08-23       Impact factor: 6.514

9.  Synthesis, Characterization, and Anti-Inflammatory Activity of Newer Quinazolinone Analogs.

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10.  Synthesis and biological evaluation of 2-aminobenzamide derivatives as antimicrobial agents: opening/closing pharmacophore site.

Authors:  Yahia N Mabkhot; Abdullah M Al-Majid; Assem Barakat; Salim S Al-Showiman; Munirah S Al-Har; Smaail Radi; Muhammad Moazzam Naseer; Taibi B Hadda
Journal:  Int J Mol Sci       Date:  2014-03-21       Impact factor: 5.923

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