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Vol.4 , No. 5, Publication Date: Aug. 31, 2017, Page: 30-35
 was synthesized. Benzimidazole nucleus was acylated in 1-position with benzoyl chloride in basic medium at room temperature to form N-acylated benzimidazole (1). Reaction of the N-acylated benzimidazole (1) with different amines yields the desired N-substituted benzimidazole derivatives (2-5). All the synthesized compounds (1-5) were evaluated in vivo for analgesic activity by acetic acid induced writhing and hot plate tests in mice. In comparison to the standard drug aspirin at the same dose (50mg/kg), compound 4 was the most potent as it decreased the number of writings to 17% comparing to control. However, aspirin resulted in a decrease equal to 12% of the control. In addition, all the test compounds except 5 produced some reduction in reaction time for hot plate test. Markedly, the effect was statistically significant with compounds 3 and 4.&picture=http://www.aascit.org/aascit/decorators/img/journal/905.jpg)
| [1] | Asma Eswayah, Department of Medicinal and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tripoli, Tripoli, Libya. |
| [2] | Souad Khaliel, Department of Chemistry, Faculty of Science, University of Benghazi, Benghazi, Libya. |
| [3] | Shaban Saad, Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, University of Tripoli, Tripoli, Libya. |
| [4] | Naima Shebani, Department of Medicinal and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tripoli, Tripoli, Libya. |
| [5] | Omran Fhid, Department of Medicinal and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tripoli, Tripoli, Libya. |
| [6] | Amal Belaid, Department of Medicinal and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tripoli, Tripoli, Libya. |
| [7] | Tawssul Alsharif, Department of Medicinal and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tripoli, Tripoli, Libya. |
| [8] | Haneen Elforjane, Department of Medicinal and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tripoli, Tripoli, Libya. |
| [9] | Yousra Saadalla, Department of Chemistry, Faculty of Science, University of Benghazi, Benghazi, Libya. |
| [10] | Ennam Baga, Department of Chemistry, Faculty of Science, University of Benghazi, Benghazi, Libya. |
A series of N-substituted benzimidazole derivatives (1-5) was synthesized. Benzimidazole nucleus was acylated in 1-position with benzoyl chloride in basic medium at room temperature to form N-acylated benzimidazole (1). Reaction of the N-acylated benzimidazole (1) with different amines yields the desired N-substituted benzimidazole derivatives (2-5). All the synthesized compounds (1-5) were evaluated in vivo for analgesic activity by acetic acid induced writhing and hot plate tests in mice. In comparison to the standard drug aspirin at the same dose (50mg/kg), compound 4 was the most potent as it decreased the number of writings to 17% comparing to control. However, aspirin resulted in a decrease equal to 12% of the control. In addition, all the test compounds except 5 produced some reduction in reaction time for hot plate test. Markedly, the effect was statistically significant with compounds 3 and 4.
Keywords
Benzimidazole, N-Acyl Benzimidazole, Analgesic Activity, Hot Plate Method, Acetic Acid Induced Writhing
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