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合成及一些新型 2-取代-4,5-二苯基咪唑类化合物的驱虫活性。

Synthesis and anthelmintic activity of some novel 2-substituted-4,5-diphenyl imidazoles.

机构信息

Department of Pharmacy, IIMT College of Medical Sciences, 'O'Pocket, Ganga Nagar, Mawana Road, Meerut-250001, Uttar, Pradesh, India.

出版信息

Acta Pharm. 2010 Jun;60(2):229-35. doi: 10.2478/v10007-010-0011-1.

Abstract

A series of 2-substituted-4,5-diphenyl imidazoles 1a-j were synthesized by refluxing benzil with different substituted aldehydes in the presence of ammonium acetate and glacial acetic acid. Structures of the synthesized compounds were confirmed on the basis of IR, 1H NMR and mass spectral data. Compounds 1a-j were screened for anthelmintic activity. Test results revealed that compounds showed paralysis time of 0.24 to 1.54 min and death time of 0.39 to 4.40 min while the standard drugs albendazole and piperazine citrate showed paralysis time of 0.54 and 0.58 min and death time of 2.16 and 2.47 min, respectively, at the same concentration of 1% (m/V). Five compounds, 2-[2-hydroxyphenyl]-4,5-diphenyl imidazole (1b), 2-[3-methoxyphenyl]-4,5-diphenyl imidazole (1c), 2-[2-phenylethenyl]-4,5-diphenyl imidazole (1e), 2-[4-fluorophenyl]-4,5-diphenyl imidazole (1g) and 2-[3-nitrophenyl]-4,5-diphenyl imidazole (1h) showed significant anthelmintic activity compared to the standard drugs.

摘要

一系列 2-取代-4,5-二苯基咪唑 1a-j 是通过将苯偶姻与不同取代的醛在醋酸铵和冰醋酸存在下回流合成的。根据红外、1H NMR 和质谱数据确认了合成化合物的结构。对合成的化合物 1a-j 进行了抗蠕虫活性筛选。测试结果表明,化合物表现出 0.24 至 1.54 分钟的麻痹时间和 0.39 至 4.40 分钟的死亡时间,而标准药物阿苯达唑和柠檬酸哌嗪在相同浓度 1%(m/V)下分别表现出 0.54 和 0.58 分钟的麻痹时间和 2.16 和 2.47 分钟的死亡时间。五种化合物,2-[2-羟基苯基]-4,5-二苯基咪唑(1b)、2-[3-甲氧基苯基]-4,5-二苯基咪唑(1c)、2-[2-苯乙烯基]-4,5-二苯基咪唑(1e)、2-[4-氟苯基]-4,5-二苯基咪唑(1g)和 2-[3-硝基苯基]-4,5-二苯基咪唑(1h)与标准药物相比表现出显著的抗蠕虫活性。

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