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某些1-苄基-2-取代-4,5-二苯基-1H-咪唑衍生物的合成与镇痛活性

Synthesis and analgesic activity of some 1-benzyl-2-substituted-4,5-diphenyl-1H-imidazole derivatives.

作者信息

Uçucu O, Karaburun N G, Işikdağ I

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Anadolu, Eskişehir, Turkey.

出版信息

Farmaco. 2001 Apr;56(4):285-90. doi: 10.1016/s0014-827x(01)01076-x.

Abstract

In this study, derivatives of 1-benzyl-2-substituted-4,5-diphenyl-1H-imidazole were synthesized and their analgesic activity assayed in two tests. 1,2,4,5-Tetrasubstituted imidazole compounds were obtained by the treatment of purified imidazole compounds with benzyl chloride in the presence of sodium hydride. The structure elucidation of the compounds was performed by IR, 1H-NMR and mass spectroscopic data and elemental analysis results. Generally the prepared compound exhibited only moderate analgesic activity in mice at the dose of 100 mg/kg i.p.; however, a few of them exhibited good activity, almost equivalent to that of morphine at 1 mg/kg i.p. was observed. At the above dosage, no toxicity was observed for all compounds.

摘要

在本研究中,合成了1-苄基-2-取代-4,5-二苯基-1H-咪唑的衍生物,并在两项试验中测定了它们的镇痛活性。通过在氢化钠存在下用苄基氯处理纯化的咪唑化合物获得了1,2,4,5-四取代咪唑化合物。通过红外光谱、1H-核磁共振和质谱数据以及元素分析结果对化合物进行结构解析。一般来说,所制备的化合物在小鼠腹腔注射剂量为100 mg/kg时仅表现出中等镇痛活性;然而,其中一些表现出良好的活性,几乎与腹腔注射1 mg/kg吗啡的活性相当。在上述剂量下,所有化合物均未观察到毒性。

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