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4-(6-甲氧基-2-萘基)丁-2-酮及相关类似物,一类新型抗炎化合物结构。

4-(6-Methoxy-2-naphthyl)butan-2-one and related analogues, a novel structural class of antiinflammatory compounds.

作者信息

Goudie A C, Gaster L M, Lake A W, Rose C J, Freeman P C, Hughes B O, Miller D

出版信息

J Med Chem. 1978 Dec;21(12):1260-4. doi: 10.1021/jm00210a016.

Abstract

A series of compounds related to 4-(6-methoxy-2-naphthyl)butan-2-one has been prepared and tested for antiinflammatory activity by the cotton pellet granuloma method. Compounds possessing a small lipophilic group such as methoxyl, methyl, or chloro in the 6 position in conjunction with a butan-2-one side chain in the 2 position of the naphthalene ring were most active. The indtroduction of a methyl group along the side chain was invariably deleterious. Good activity was generally retained by forming esters of a butan-2-ol side chain.

摘要

已经制备了一系列与4-(6-甲氧基-2-萘基)丁-2-酮相关的化合物,并通过棉球肉芽肿法测试了它们的抗炎活性。在萘环2位带有丁-2-酮侧链的同时,6位带有小的亲脂性基团如甲氧基、甲基或氯的化合物活性最高。沿着侧链引入甲基总是有害的。通过形成丁-2-醇侧链的酯,通常能保持良好的活性。

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