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Synthesis and anti-liver fibrosis activity of imidazole and thiazole compounds containing amino acids.
Meng, Yu-Qing; Ren, Jie; Sun, Jing-Xin; Guo, Fang-Yan; Min, Jun-Zhe; Nan, Ji-Xing; Quan, Ji-Shan; Lian, Li-Hua; Jin, Cheng-Hua.
Affiliation
  • Meng YQ; Interdisciplinary Program of Biological Function Molecules, College of Integration Science, Yanbian University, Yanji, 133002, China.
  • Ren J; Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, 133002, China.
  • Sun JX; Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, 133002, China.
  • Guo FY; Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, 133002, China.
  • Min JZ; Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, 133002, China.
  • Nan JX; Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, 133002, China; Interdisciplinary Program of Biological Function Molecules, College of Integration Science, Yanbian University, Yanji, 133002, China.
  • Quan JS; Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, 133002, China; Interdisciplinary Program of Biological Function Molecules, College of Integration Science, Yanbian University, Yanji, 133002, China. Electronic address
  • Lian LH; Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, 133002, China; Interdisciplinary Program of Biological Function Molecules, College of Integration Science, Yanbian University, Yanji, 133002, China. Electronic address
  • Jin CH; Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, 133002, China; Interdisciplinary Program of Biological Function Molecules, College of Integration Science, Yanbian University, Yanji, 133002, China. Electronic address
Eur J Med Chem ; 269: 116311, 2024 Apr 05.
Article in En | MEDLINE | ID: mdl-38508118
ABSTRACT
Four series of imidazoles (15a-g, 20c, and 20d) and thiazoles (18a-g, 22a, and 22b) possessing various amino acids were synthesized and evaluated for activin receptor-like kinase 5 (ALK5) inhibitory activities in an enzymatic assay. Among them, compounds 15g and 18c showed the highest inhibitory activity against ALK5, with IC50 values of 0.017 and 0.025 µM, respectively. Compounds 15g and 18c efficiently inhibited extracellular matrix (ECM) deposition in TGF-ß-induced hepatic stellate cells (HSCs), and eventually suppressed HSC activation. Moreover, compound 15g showed a good pharmacokinetic (PK) profile with a favorable half-life (t1/2 = 9.14 h). The results indicated that these compounds exhibited activity targeting ALK5 and may have potential in the treatment of liver fibrosis; thus they are worthy of further study.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiazoles / Amino Acids Limits: Humans Language: En Journal: Eur J Med Chem Year: 2024 Document type: Article Affiliation country: Country of publication:
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiazoles / Amino Acids Limits: Humans Language: En Journal: Eur J Med Chem Year: 2024 Document type: Article Affiliation country: Country of publication: