Synthesis and pharmacological evaluation of derivatives structurally related to nimesulide

被引：21

作者：

Cignarella, G ^{[1
]}

Vianello, P ^{[1
]}

Berti, F ^{[1
]}

Rossoni, G ^{[1
]}

机构：

[1] DIPARTIMENTO FARMACOL CHEMIOTERAPIA & TOSSICOL ME,I-20129 MILAN,ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 31卷 / 05期

关键词：

nimesulide; antiinflammatory-antihistaminic activity; N-pyridinyl analogue;

D O I：

10.1016/0223-5234(96)89162-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present work reports the synthesis of a series of compounds structurally related to the antiinflammatory and antihistaminic agent nimesulide (I), in which the p-nitrophenyl moiety has been replaced by pyridine (1a-c) and pyridine N-oxide (2a-c). In addition, two compounds (3a, 4a) have been synthesized in which the p-nitro group of I was substituted by a cyano and a 1H-tetrazol-5-yl group, respectively. Representative 1a and 2a were also modified by replacing the methanesulfonamido group with an acetamido group (5a, 6a). The pharmacological evaluation of compounds 1-6 in comparison to I, indicates that such modifications are detrimental to the activity. Moreover 3a and 4a caused bronchoconstriction and hypotension, thus behaving as histaminic-like rather then antihistaminic agents.

引用

页码：359 / 364

页数：6

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