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Design, Synthesis, and Biological Evaluation of a Novel Series of 4-Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity

[Image: see text] To discover a novel series of potent inhibitors of enteropeptidase, a membrane-bound serine protease localized to the duodenal brush border, 4-guanidinobenzoate derivatives were evaluated with minimal systemic exposure. The 1c docking model enabled the installation of an additional...

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Detalles Bibliográficos
Autores principales: Ikeda, Zenichi, Kakegawa, Keiko, Kikuchi, Fumiaki, Itono, Sachiko, Oki, Hideyuki, Yashiro, Hiroaki, Hiyoshi, Hideyuki, Tsuchimori, Kazue, Hamagami, Kenichi, Watanabe, Masanori, Sasaki, Masako, Ishihara, Youko, Tohyama, Kimio, Kitazaki, Tomoyuki, Maekawa, Tsuyoshi, Sasaki, Minoru
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9234964/
https://www.ncbi.nlm.nih.gov/pubmed/35686954
http://dx.doi.org/10.1021/acs.jmedchem.2c00463