62150-47-4Relevant articles and documents
Synthesis and biological evaluation of 1,3,4-oxadiazole fused pyridine derivatives as antibacterial and antifungal agents
Subhashini,Bhadraiah,Janaki
, p. 550 - 553 (2017)
A series of novel 1,3,4-oxadiazole fused pyridine derivatives were synthesized 11a–11f and their structures confirmed by IR, 1H NMR and Mass spectral data. The compounds were evaluated for their antibacterial and antifungal activities against Gram negative and positive bacterial strains including Escherichia coli (MTCC 443), K. Pneumoniae (MTCC 109), S. Aureus (MTCC 96), B. Subtilis (MTCC 441) and Sclerotium rolfsii, Macrophomina phaseolina. Compounds 11d, 11e, and 11f demonstrated high antibacterial activity.
Structure-activity relationship studies for the development of inhibitors of murine adipose triglyceride lipase (ATGL)
Breinbauer, Rolf,Doler, Carina,Fuchs, Elisabeth,Grabner, Gernot F.,Mayer, Nicole,Melcher, Michaela-Christina,Migglautsch, Anna K.,Romauch, Matthias,Schweiger, Martina,Zechner, Rudolf,Zimmermann, Robert
, (2020/07/13)
High serum fatty acid (FA) levels are causally linked to the development of insulin resistance, which eventually progresses to type 2 diabetes and non-alcoholic fatty liver disease (NAFLD) generalized in the term metabolic syndrome. Adipose triglyceride lipase (ATGL) is the initial enzyme in the hydrolysis of intracellular triacylglycerol (TG) stores, liberating fatty acids that are released from adipocytes into the circulation. Hence, ATGL-specific inhibitors have the potential to lower circulating FA concentrations, and counteract the development of insulin resistance and NAFLD. In this article, we report about structure–activity relationship (SAR) studies of small molecule inhibitors of murine ATGL which led to the development of Atglistatin. Atglistatin is a specific inhibitor of murine ATGL, which has proven useful for the validation of ATGL as a potential drug target.
2 - Amino - 4 - bromo pyridine synthesis method
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Paragraph 0059; 0060-0061, (2018/04/26)
The invention relates to the field of medical intermediate synthesis, in particular to a synthetic method of 2-amino-4-bromopyridine, and provides a preparation method of 2-amino-4-bromopyridine. The preparation method comprises the following steps: (1) esterification reaction: esterifying 4-bromopyridinium chloride to obtain a 4-bromopyridine-2-ethyl formate crude product; (2) ammoniation reaction: ammonifying the 4-bromopyridine-2-ethyl formate crude product into 4-bromopyridine-2-formamide; (3) Hofmann degradation reaction: conducting Hofmann degradation on 4-bromopyridine-2-formamide to obtain 2-amino-4-bromopyridine, wherein the synthetic route is shown in the formula I. The synthetic method provided by the invention has the advantages that the raw material cost is low; the yield is high; the reactions and the operation are simple; the three waste treatment is convenient; industrialization can be realized easily.