In this study, we have made an attempt to synthesize novel imidazole derivatives (2a-h) and evaluate them for anticonvulsant activity using maximal electroshock method (MES). In the first step, substituted amines were allowed to react with substituted benzaldehyde in an equimolar amount with glacial acetic acid to form various substituted Schiff's base intermediate (1a-h). Schiff's base on treatment with benzil in the presence of ammonium acetate afforded corresponding imidazole derivatives (2a-h). The structure of the final analogs has been confirmed on the basis of elemental analysis, Fourier transform infrared spectroscopy (FT-IR), H-1 nuclear magnetic resonance (NMR), C-13 NMR, and mass spectra. Among all synthesized compounds, compounds 2a, 2f, and 2b were found to be most potent in comparison with standard phenytoin. [GRAPHICS]
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Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Lv, Peng-Cheng
Wang, Kai-Rui
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Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Wang, Kai-Rui
Yang, Ying
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Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Yang, Ying
Mao, Wen-Jun
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Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Mao, Wen-Jun
Chen, Jin
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Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Chen, Jin
Xiong, Jing
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Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
Xiong, Jing
Zhu, Hai-Liang
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Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R ChinaNanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Peoples R China
机构:
King Khalid Univ, Res Ctr Adv Mat Sci RCAMS, Chem Dept, Fac Sci, PO Box 9004, Abha 61413, Saudi ArabiaIslamia Univ Bahawalpur, Inst Chem, Bahawalpur 63100, Pakistan
Ismail, Mostafa A.
Najam, Tayyaba
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SciTech Int Pvt Ltd, Res & Dev Div, G 10-1, Islamabad, PakistanIslamia Univ Bahawalpur, Inst Chem, Bahawalpur 63100, Pakistan
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Fujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
Xu, Shaohua
Fan, Ruolan
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Fujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
Fan, Ruolan
Wang, Lu
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Nanjing Univ Chinese Med, Natl Ctr Colorectal Dis, Nanjing Hosp Chinese Med, 157 Daming Rd, Nanjing 210022, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
Wang, Lu
He, Weishen
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Boston Coll, Biol Dept, Brighton, MA USAFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
He, Weishen
Ge, Haixia
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Huzhou Univ, Sch Life Sci, Huzhou, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
Ge, Haixia
Chen, Hailan
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Fujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
Chen, Hailan
Xu, Wen
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Fujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
Xu, Wen
Zhang, Jian
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China Pharmaceut Univ, State Key Lab Nat Med, Nanjing, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
Zhang, Jian
Xu, Wei
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Fujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
Xu, Wei
Feng, Yaqian
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Tsinghua Univ, Sch Pharmaceut Sci, Key Lab Bioorgan Phosphorus Chem & Chem Biol, Minist Educ, Beijing, Peoples R China
Tsinghua Univ, Sch Pharmaceut Sci, 30 Shuangqing Rd, Beijing 100084, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China
Feng, Yaqian
Fan, Zhimin
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Nanjing Univ Chinese Med, Natl Ctr Colorectal Dis, Nanjing Hosp Chinese Med, 157 Daming Rd, Nanjing 210022, Peoples R ChinaFujian Univ Tradit Chinese Med, Coll Pharm, 1 Qiuyang Rd, Fuzhou 350122, Peoples R China