Product Details of 148-51-6. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloride, is researched, Molecular C8H12ClNO2, CAS is 148-51-6, about Inhibition of colitis by ring-modified analogues of 6-acetamido-2,4,5-trimethylpyridin-3-ol.
6-Aminopyridin-3-ol scaffold has shown an excellent anti-inflammatory bowel disease activity. Various analogs with the scaffold were synthesized in pursuit of the diversity of side chains tethering on the C(6)-position. SAR among the analogs was investigated to understand the effects of the side chains and their linkers on their anti-inflammatory activities. In this study, structural modification moved beyond side chains on the C(6)-position and reached to pyridine ring itself. It expedited to synthesize diverse ring-modified analogs of a representative pyridine-3-ol, 6-acetamido-2,4,5-trimethylpyridin-3-ol. In the evaluation of compounds on their inhibitory actions against TNF-α-induced adhesion of monocytic cells to colonic epithelial cells, an in vitro model mimicking colon inflammation, the effects of compounds I , II, and III were greater than tofacitinib, an orally available anti-colitis drug, and compound dehydroxylated analog II exhibit the greatest activity. In addition, TNF-α-induced angiogenesis, which permits more inflammatory cell migration into inflamed tissues, was significantly blocked by compounds I and II in a concentration-dependent manner. In the comparison of in vivo therapeutic effects of compounds I , II, and III on dextran sulfate sodium (DSS)-induced colitis in mice, compound dehydroxylated analog II was the most potent and efficacious, and compound demethylated analog III was better than compound I which exhibited a similar degree of inhibitory effect to tofacitinib.
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Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia