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新型4-(4-取代芳基)氨基脲类抗惊厥剂的设计与合成

Design and Synthesis of Some Novel 4-(4-substituted aryl) Semicarbazones as Anticonvulsant Agents.

作者信息

Singh Anita, Pande C, Gahtori P, Pandeya S N, Stables J P

机构信息

Department of Pharmacy, Kumaun University, Bhimtal-263 002, India.

出版信息

Indian J Pharm Sci. 2010 May;72(3):363-7. doi: 10.4103/0250-474X.70485.

Abstract

In the present study, a series of 4-(4-substituted aryl) semicarbazones were synthesized from substituted anilines and subsequently evaluated for their anticonvulsant activities. The anticonvulsant activities were established by the anticonvulsant drug development (ADD) programme NIH, USA using experimental animal, adult male FCM mice (20-25 g) and adult Sprague-Dawley rats (100-150 g) and screened against electroshock seizure, subcutaneous metrazole and minimal neurotoxicity tests in mice. Compound 7 was found equipotent to carbamazepine in both MES and ScPTZ tests. This study has highlighted the importance of distal alkyl chain which influences the anticonvulsant activity.

摘要

在本研究中,由取代苯胺合成了一系列4-(4-取代芳基)氨基脲,随后对其抗惊厥活性进行了评估。抗惊厥活性由美国国立卫生研究院的抗惊厥药物开发(ADD)计划使用实验动物、成年雄性FCM小鼠(20 - 25克)和成年斯普拉格-道利大鼠(100 - 150克)确定,并针对小鼠的电休克惊厥、皮下注射戊四氮和最小神经毒性试验进行筛选。在最大电休克(MES)和皮下注射戊四氮(ScPTZ)试验中,发现化合物7与卡马西平具有同等效力。本研究突出了影响抗惊厥活性的远端烷基链的重要性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f616/3003172/934cb4fc0368/IJPhS-72-363-g001.jpg

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