Name: 4-Hydroxypicolinic acid. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 4-Hydroxypicolinic acid, is researched, Molecular C6H5NO3, CAS is 22468-26-4, about Discovery of a novel azetidine scaffold for colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors by the use of docking models. Author is Ikegashira, Kazutaka; Ikenogami, Taku; Yamasaki, Takayuki; Hase, Yasunori; Yamaguchi, Takayuki; Inagaki, Koji; Doi, Satoki; Adachi, Tsuyoshi; Koga, Yoshihisa; Hashimoto, Hiromasa.
We report the discovery of a novel azetidine scaffold for colony stimulating factor-1 receptor (CSF-1R) Type II inhibitors by using a structure-based drug design (SBDD) based on a docking model. The work leads to the representative compound 4a with high CSF-1R inhibitory activity (IC50 = 9.1 nM). The obtained crystal structure of an azetidine compound with CSF-1R, which matched our predicted docking model, demonstrates that the azetidine compounds bind to the DFG-out conformation of the protein as a Type II inhibitor.
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