Synthesis and In vivo Antifibrotic Activity of Novel Leflunomide Analogues

被引：9
|
作者：
Hamdi, Abdelrahman [1 ]
Said, Eman [2 ]
Farahat, Abdelbasset A. [1 ]
El-Bialy, Serry A. A. [1 ]
Massoud, Mohammed A. M. [1 ]
机构：
[1] Mansoura Univ, Pharmaceut Organ Chem Dept, Fac Pharm, Mansoura 35516, Egypt
[2] Mansoura Univ, Pharmacol & Toxicol Dept, Fac Pharm, Mansoura 35516, Egypt
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2016年 / 13卷 / 09期
关键词：
Leflunomide; cirrhosis; antifibrotic; isoxazole; LIVER FIBROSIS; HEPATITIS; CIRRHOSIS; PROLIFERATION; METABOLITE; CELLS; RATS;
D O I：
10.2174/1570180813666160630125624
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel Leflunomide analogues were synthesized and evaluated in vivo against thioacetamide (TAA) induced liver fibrosis in rats. All the animals which were treated with the new analogues showed improved or comparable survival rates to those treated with Leflunomide. Animals which were treated with compounds 8d, 8e, 9 and 11 have shown improved liver parameters than Leflunomide treated animals. Histopathology of the liver has shown that compound 8a is the most active compound, which decreases fibrosis to a minimal level and compounds 8c, 8e and 11 are active compounds with fibrosis score 2-3 which is better than that of Leflunomide.
引用
收藏
页码：912 / 920
页数：9
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