Synthesis and In vivo Antifibrotic Activity of Novel Leflunomide Analogues

Author(s): Abdelrahman Hamdi, Eman Said, Abdelbasset A. Farahat, Serry A. A. El-Bialy, Mohammed A. M. Massoud

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 9 , 2016

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Graphical Abstract:


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.

Keywords: Leflunomide, cirrhosis, antifibrotic, isoxazole.

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Article Details

Year: 2016
Page: [912 - 920]
Pages: 9
DOI: 10.2174/1570180813666160630125624
Price: $65

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