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使用 2,6-二取代烟酰基肼研究一些吡啶衍生物的抗炎、镇痛、抗惊厥和抗帕金森活性。

Anti-inflammatory, analgesic, anticonvulsant and antiparkinsonian activities of some pyridine derivatives using 2,6-disubstituted isonicotinic acid hydrazides.

机构信息

Department of Pharmaceutical Chemistry, King Saud University, Riyadh, Saudi Arabia.

出版信息

Arch Pharm (Weinheim). 2010 Nov;343(11-12):648-56. doi: 10.1002/ardp.201000088.

Abstract

A series of novel thiazolo derivatives 2-15 was synthesized by initial condensation of 2,6-dihydroxyisonicotinohydrazide 1 and 2-chloro-6-hydrazinylisonicotinohydrazide 11 with different organic reagents. The pharmacological screening showed that many of these obtained compounds have good anti-inflammatory, analgesic, anticonvulsant, and antiparkinsonian activities comparable to diclofenac potassium, Voltarene(®), Carbamazepine(®), and Benzotropene(®) as reference drugs. Initially the acute toxicity of the compounds was assayed via the determination of their LD₅₀. The structures of newly synthesized compounds were confirmed by IR, ¹H-NMR, ¹³C-NMR, MS spectral data and elemental analysis. The detailed synthesis, spectroscopic data, LD₅₀ and pharmacological activities of the synthesized compounds were reported.

摘要

通过 2,6-二羟基异烟酰肼 1 和 2-氯-6-肼基异烟酰肼 11 与不同有机试剂的初始缩合,合成了一系列新型噻唑啉衍生物 2-15。药理筛选表明,这些获得的化合物中的许多具有良好的抗炎、镇痛、抗惊厥和抗帕金森病活性,与双氯芬酸钾、Voltaren(®)、卡马西平(®)和苯托品(®)作为参考药物相当。最初通过测定化合物的 LD₅₀来测定其急性毒性。新合成化合物的结构通过 IR、¹H-NMR、¹³C-NMR、MS 谱数据和元素分析得到确认。报道了合成化合物的详细合成、光谱数据、LD₅₀ 和药理学活性。

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