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新型酰肼和肼衍生物的合成及其镇痛活性

Synthesis and analgesic activity of novel hydrazide and hydrazine derivatives.

作者信息

Nassiri Koopaei Mansur, Assarzadeh Mohammad Javad, Almasirad Ali, Ghasemi-Niri Seyedeh Farnaz, Amini Mohsen, Kebriaeezadeh Abbas, Nassiri Koopaei Nasser, Ghadimi Maryam, Tabei Arash

机构信息

Department of Medicinal Chemistry, Pharmaceutical Sciences branch, Islamic Azad University, Tehran, Iran.

Department of Pharmacology and Toxicology, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Iran J Pharm Res. 2013 Fall;12(4):721-7.

Abstract

The uses of non-steroidal anti-inflammatory drugs (NSAIDs) are limited by a variety of side effects. So research on preparing new analgesic agents is important. According to some reports about the analgesic activity of hydrazide and hydrazine derivatives a new series of these compounds were synthesized in order to obtain new analgesic compounds. The final compounds 10a-10e and 15a-15d were prepared by condensation of corresponding hydrazides 7,8 and 11-14 with different aldehydes 9a-9e. The structures of all synthesized compounds were confirmed by means of FT-IR, 1H-NMR and Mass spectra. All compounds were evaluated for their analgesic activities by abdominal constriction test (writhing test). Most of the synthesized compounds induced significant reduction in the writhing response when compared to control and compound 15 was more potent than mefenamic acid in the writhing test.

摘要

非甾体抗炎药(NSAIDs)的使用受到多种副作用的限制。因此,制备新型镇痛剂的研究具有重要意义。根据一些关于酰肼和肼衍生物镇痛活性的报道,合成了一系列此类新化合物以获得新型镇痛化合物。最终化合物10a - 10e和15a - 15d是通过相应的酰肼7、8和11 - 14与不同的醛9a - 9e缩合制备而成。所有合成化合物的结构均通过傅里叶变换红外光谱(FT - IR)、核磁共振氢谱(1H - NMR)和质谱进行了确证。所有化合物均通过腹部收缩试验(扭体试验)评估其镇痛活性。与对照相比,大多数合成化合物在扭体反应中引起显著降低,并且化合物15在扭体试验中比甲芬那酸更有效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bee/3920700/48f33c770650/ijpr-12-721-g001.jpg

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