Category: alcohols-buliding-blocks《Inhibition of colitis by ring-modified analogues of 6-acetamido-2,4,5-trimethylpyridin-3-ol》 was published in 2020. The authors were Chaudhary, Chhabi Lal;Chaudhary, Prakash;Dahal, Sadan;Bae, Dawon;Nam, Tae-gyu;Kim, Jung-Ae;Jeong, Byeong-Seon, and the article was included in《Bioorganic Chemistry》. The author mentioned the following in the article:
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. And 5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloride (cas: 148-51-6) was used in the research process.
5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloride(cas:148-51-6 Category: alcohols-buliding-blocks) is a strong antagonist of vitamin B6. Deoxypyridoxine hydrochloride has been used as an analytical reference standard for the quantification of the analyte in food samples using high performance liquid chromatography.
Reference:
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