A new class of ibuprofen derivatives with reduced gastrotoxicity

被引:70
作者
Lolli, ML
Cena, C
Medana, C
Lazzarato, L
Morini, G
Coruzzi, G
Manarini, S
Fruttero, R
Gasco, A
机构
[1] Univ Turin, Dipartimento Sci & Tecnol Farm, I-10125 Turin, Italy
[2] Univ Parma, Ist Farmacol, I-43100 Parma, Italy
[3] Ist Ric Farmacol Mario Negri, Consorzio Mario Negri Sud, Lab Interaz Tra Cellule Emat & Vasc, Dipartimento Med & Farmacol Vasc, I-66030 Santa Maria Imbaro, CH, Italy
关键词
D O I
10.1021/jm0108799
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new series of nonsteroidal and inflammatory drugs (NSAIDs) obtained by linking ibuprofen to selected furoxan moieties and to related furazans were synthesized and tested for their antiinflammatory, antiaggregatory, and ulcerogenic properties. All the derivatives are endowed with antiinflammatory activity comparable to that of ibuprofen, but, unlike this drug, they display reduced acute gastrotoxicity. The masking of the ibuprofen-free carboxylic group seems to be principally at the basis of this reduced topical irritant action. The two furoxan derivatives 8 and 9 also trigger potent antiaggregatory effects, principally as a consequence of their NO-donor ability.
引用
收藏
页码:3463 / 3468
页数:6
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