一些新型2,5-二取代-1,3,4-噻二唑的合成与抗惊厥活性评价：药效团模型研究
Synthesis and anticonvulsant evaluation of some novel 2,5-disubstituted 1,3,4-thiadiazoles: pharmacophore model studies.
作者信息
Rajak Harish, Behera Chinmay Kumar, Pawar Rajesh Singh, Singour Pradeep Kumar, Kharya Murli Dhar
机构信息
Medicinal Chemistry Research Laboratory, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur-495 009, India.
出版信息
Acta Pol Pharm. 2010 Sep-Oct;67(5):503-10.
A novel series of N'-{5-[(1H-indol-3-ylmethyl)-1,3,4-thiadiazol-2-yl}-N4-(4-substituted benzaldehyde)-semicarbazones, N1-{5-[(1H-indol-3-ylmethyl)-1,3,4-thiadiazol-2-yl}-N4-[1-(4-substituted phenyl)ethanone]-semicarbazones and N1-{5-[(1H-indol-3-ylmethyl)-1,3,4-thiadiazol-2-yl}-N4-[1-(4-substituted phenyl) (phenyl) methanone]-semicarbazones were synthesized and evaluated for their anticonvulsant potential using maximal electroshock seizure (MES) and subcutaneous pentylenetrtrazole (scPFZ) models. The minimal motor impairment (neurotoxicity) was determined by rotorod test. The results of the present study confirmed the requirements of various structural features of four binding site pharmacophore model for anticonvulsant activity.
合成了一系列新型的N'-{5-[(1H-吲哚-3-基甲基)-1,3,4-噻二唑-2-基}-N4-(4-取代苯甲醛)-氨基脲、N1-{5-[(1H-吲哚-3-基甲基)-1,3,4-噻二唑-2-基}-N4-[1-(4-取代苯基)乙酮]-氨基脲和N1-{5-[(1H-吲哚-3-基甲基)-1,3,4-噻二唑-2-基}-N4-[1-(4-取代苯基)(苯基)甲酮]-氨基脲，并使用最大电休克惊厥（MES）和皮下注射戊四氮（scPTZ）模型评估了它们的抗惊厥潜力。通过转棒试验确定最小运动损伤（神经毒性）。本研究结果证实了抗惊厥活性的四结合位点药效团模型的各种结构特征的要求。
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