Synthesis and evaluation of the anti-inflammatory effects of niflumic acid lipophilic prodrugs in brain edema

被引：0

作者：

ElKihel, L

Bourass, J

Richomme, P

Petit, JY

Letourneux, Y

机构：

[1] UNIV LA ROCHELLE,LABS SESNAB,F-17042 LA ROCHELLE,FRANCE

[2] FAC PHARM ANGERS,LAB PHARMACOGNOSIE,ANGERS,FRANCE

[3] FAC PHARM,PHARMACOL LAB,NANTES,FRANCE

来源：

ARZNEIMITTEL-FORSCHUNG/DRUG RESEARCH | 1996年 / 46卷 / 11期

关键词：

anti-inflammatories; blood-brain barrier; lipophilic prodrugs; non-steroidal; CAS; 4394-00-7; niflumic acid; Nifluril(R);

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Five new lipophilic prodrugs of the non-steroidal anti-inflammatory drug, niflumic acid (Nifluril(R), CAS 4394-00-7). were synthetized and evaluated on the experimental brain edema (injection of phospholipase A(2)). The effect of these drugs in comparison with dexamethasone which elicits a marked effect on clinical and experimental brain edema was evaluated. Niflumic acid was vectorised by cholesterol, hexadecanol and by three 1,3-diacylglycerols. The anti-inflammatory activity of these compounds on experimental brain edema was evaluated by determination of the prostaglandin E(2) (PGE(2)) brain tissue concentration. Niflumic acid reduced the prostaglandin E(2) production more significantly than dexamethasone. Niflumic acid prodrug forms (1,3-dihexadecanoyl-2-[2-[3-(trifluoromethyl)anilino]nicotinoyl]glycerol and 1,3-dihexadecanoyl-2-[2-[3-(trifluoromethyl)anilino]nicotinoyloxybutanoyl]glycerol also showed a marked anti-inflammatory activity at low concentrations.

引用

页码：1040 / 1044

页数：5

共 15 条

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