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作为药物制剂的N-三氟乙酰衍生物。IV——抗炎及相关特性;某些多芳基三氟乙酰胺的抗菌活性。

N-trifluoroacetyl derivatives as pharmacological agents. IV--Antiinflammatory and related properties; antimicrobial activity of some polyaromatic trifluoroacetamides.

作者信息

Vigorita M G, Previtera T, Trovato A, Monforte M T, Barbera R, Bisignano G

机构信息

Dipartimento Farmaco-Chimico, Facoltà Di Farmacia, Università Di Messina, Italy.

出版信息

Farmaco. 1989 Feb;44(2):173-84.

PMID:2775414
Abstract

Taking into account both the analogy with the antiinflammatory triflamides and our previous observations on a series of trifluoroacetanilides active as acute and chronic antiinflammatory agents, the present series of polyaromatic N-trifluoroacetylderivatives were prepared. Their antiinflammatory and related properties as well as antimicrobial activity were evaluated. Few derivatives were found to display significant analgesic effects (hot plate test) whereas at 50 mg/kg all were devoid of antiinflammatory effects except the benzophenone derivative (III). Instead as regards the antimicrobial screening, a selective antimycoplasmal activity was revealed in six out of ten examined compounds.

摘要

考虑到与抗炎三氟甲磺酰胺的类比以及我们先前对一系列作为急性和慢性抗炎剂的三氟乙酰苯胺的观察结果,制备了本系列多芳族N-三氟乙酰衍生物。对它们的抗炎及相关性质以及抗菌活性进行了评估。发现很少有衍生物显示出显著的镇痛作用(热板试验),而在50mg/kg剂量下,除二苯甲酮衍生物(III)外,所有衍生物均无抗炎作用。相反,在抗菌筛选方面,在所检测的十种化合物中有六种显示出选择性抗支原体活性。

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