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
相关论文
共 50 条
  • [31] Synthesis and in vitro antitrypanosomal activity of novel Nifurtimox analogues
    Pozas, R
    Carballo, J
    Castro, C
    Rubio, J
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (05) : 1417 - 1421
  • [32] Design, synthesis, and anticonvulsant activity of novel quinazolinone analogues
    Gawad, Nagwa M. Abdel
    Georgey, Hanan Hanna
    Youssef, Riham M.
    El Sayed, Nehad A.
    MEDICINAL CHEMISTRY RESEARCH, 2011, 20 (08) : 1280 - 1286
  • [33] Synthesis of novel psoralen analogues and their in vitro antitumor activity
    Francisco, Carla S.
    Rodrigues, Ligia R.
    Cerqueira, Nuno M. F. S. A.
    Oliveira-Campos, Ana M. F.
    Rodrigues, Ligia M.
    Esteves, Ana P.
    BIOORGANIC & MEDICINAL CHEMISTRY, 2013, 21 (17) : 5047 - 5053
  • [34] Antifibrotic effects of a novel pirfenidone derivative in vitro and in vivo
    Ma, Zhen
    Zhao, Cungang
    Chen, Qi
    Yu, Chenhuan
    Zhang, Huanhuan
    Zhang, Zhimin
    Huang, Wenhai
    Shen, Zhengrong
    PULMONARY PHARMACOLOGY & THERAPEUTICS, 2018, 53 : 100 - 106
  • [35] In vivo activity of leflunomide - Pharmacokinetic analyses and mechanism of immunosuppression
    Chong, ASF
    Huang, W
    Liu, W
    Luo, JL
    Shen, JK
    Xu, W
    Ma, LL
    Blinder, L
    Xiao, F
    Xu, XL
    Clardy, C
    Foster, P
    Williams, JA
    TRANSPLANTATION, 1999, 68 (01) : 100 - 109
  • [36] Synthesis and germination activity study of novel strigolactam/strigolactone analogues
    Ge, Yuhua
    Chen, Xingyue
    Khan, Shah Nawaz
    Jia, Shuhe
    Chen, Gang
    TETRAHEDRON LETTERS, 2023, 115
  • [37] Design, synthesis and evaluation of biological activity of novel fasudil analogues
    Li, Hang
    Wang, Donghua
    Liu, Shuai
    Sun, Changhai
    Chen, Meizhu
    Wang, Xinran
    Chen, Ligong
    PHARMAZIE, 2014, 69 (12): : 867 - 873
  • [38] A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity
    Ramirez-Villalva, Alejandra
    Gonzalez-Calderon, Davir
    Gonzalez-Romero, Carlos
    Morales-Rodriguez, Macario
    Jauregui-Rodriguez, Bertha
    Cuevas-Yanez, Erick
    Fuentes-Benites, Aydee
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2015, 97 : 275 - 279
  • [39] Design, Synthesis, and Anticancer Activity of Novel Fused Purine Analogues
    Hassan, A. Y.
    Sarg, M. T.
    Bayoumi, A. H.
    Kalaf, F. G. A.
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 2017, 54 (06) : 3458 - 3470
  • [40] Synthesis and immunomodulatory activity of novel amino acid analogues of fluoxetine
    Talati, Mamta N.
    Vemireddy, Sravanthi
    Seelam, Siva Deepthi
    Halmuthur, M. Sampath Kumar
    SYNTHETIC COMMUNICATIONS, 2023, 53 (10) : 731 - 743
12345