局部抗炎药的研究。II. 含硫部分的21-取代皮质类固醇的合成及血管收缩活性

Studies on topical antiinflammatory agents. II. Synthesis and vasoconstrictive activity of 21-substituted corticosteroids with sulfur-containing moieties.

作者信息

Mitsukuchi M, Ikemoto T, Taguchi M, Higuchi S, Abe S, Yasui H, Hatayama K, Sota K

出版信息

Chem Pharm Bull (Tokyo). 1989 Jul;37(7):1795-801. doi: 10.1248/cpb.37.1795.

DOI:10.1248/cpb.37.1795

Abstract

As part of the search for new topical antiinflammatory agents, various 21-substituted corticosteroids having sulfur-containing moieties were prepared and tested for vasoconstrictive activity in humans. A structure-activity relationship study revealed that substitution of the 21-hydroxy group with a lower alkyl-thio group enhanced the activity. The activities of the 21-methylthio (3Ad) and the 21-ethylthio (3Ae) compounds were more potent than that of 9 alpha-fluoro-11 beta,21-dihydroxy-16 beta-methyl-17 alpha-valeroyloxy-1,4- pregnadiene-3,20-dione (betamethasone 17-valerate, BV).

摘要

作为寻找新型局部抗炎药的一部分，制备了各种含硫部分的21-取代皮质类固醇，并对其在人体中的血管收缩活性进行了测试。结构-活性关系研究表明，用低级烷硫基取代21-羟基可增强活性。21-甲硫基（3Ad）和21-乙硫基（3Ae）化合物的活性比9α-氟-11β，21-二羟基-16β-甲基-17α-戊酰氧基-1,4-孕二烯-3,20-二酮（倍他米松17-戊酸酯，BV）更强。

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