The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Amino-2-fluoropyridine( cas:1827-27-6 ) is researched.Recommanded Product: 1827-27-6.Wu, Jing-wei; Yin, Ling; Liu, Yu-qiang; Zhang, Huan; Xie, Ya-fei; Wang, Run-ling; Zhao, Gui-long published the article 《Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout》 about this compound( cas:1827-27-6 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: bromonaphthylmethyltriazolyl thioether preparation URAT1 inhibitor; structure bromonaphthylmethyltriazolyl thioether inhibition uric acid transporter; pharmacophore determination bromonaphthylmethyltriazolyl thioether URAT1 inhibition QSAR; 3D-QSAR; Bioisosteres; Biological evaluation; Gout; Synthesis. Let’s learn more about this compound (cas:1827-27-6).
Bromonaphthylmethyltriazolyl thioether lesinurad analogs and bioisosteres such as I were prepared as inhibitors of uric acid transporter 1 (URAT1) for potential use in treating hyperuricemia and gout. I inhibited URAT1 with an IC50 value of 32 nM, 225-fold lower than lesinurad. The pharmacophore for the lesinurad analogs was determined using a 3D-QSAR pharmacophore model; the hypothesis was validated by three methods (cost anal., Fisher’s randomization and leave-one-out).
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