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异烟肼缩杂环 6-取代 1,2,4-三唑并[3,4-b]-1,3,4-噻二唑和 1,3,4-噁二唑衍生物的合成与药理学评价。

Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole and 1,3,4-oxadiazole derivatives of isoniazid.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi 110062, India.

出版信息

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4762-5. doi: 10.1016/j.bmcl.2010.06.125. Epub 2010 Jun 27.

Abstract

The significance of this study was to prepare various isoniazid derivatives by introducing the isoniazid core into several molecules to explore the possibilities of some altered biological activities. Series of 6-substituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (3a-g) and 1,3,4-oxadiazole (4a-g and 5) derivatives of isoniazid were synthesized in satisfactory yield and pharmacologically evaluated for their anti-inflammatory, analgesic, ulcerogenic, and lipid peroxidation activities by known experimental models.

摘要

本研究的意义在于通过将异烟肼核心引入几种分子中,制备各种异烟肼衍生物,以探索一些改变的生物活性的可能性。本研究合成了一系列 6-取代-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑(3a-g)和异烟肼的 1,3,4-噁二唑(4a-g 和 5)衍生物,以已知的实验模型评估其抗炎、镇痛、致溃疡和脂质过氧化活性。

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