In 2022,Sutherland, Hamish S.; Lu, Guo-Liang; Tong, Amy S. T.; Conole, Daniel; Franzblau, Scott G.; Upton, Anna M.; Lotlikar, Manisha U.; Cooper, Christopher B.; Palmer, Brian D.; Choi, Peter J.; Denny, William A. published an article in European Journal of Medicinal Chemistry. The title of the article was 《Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis》.Quality Control of Methyl 5-bromopicolinate The author mentioned the following in the article:
Drug resistant tuberculsosis (TB) is global health crisis that demands novel treatment strategies. Bacterial ATP synthase inhibitors such as bedaquiline and next-generation analogs (such as TBAJ-876) have shown promising efficacy in patient populations and preclin. studies, resp., suggesting that selective targeting of this enzyme presents a validated therapeutic strategy for the treatment of TB. In this work, we report tetrahydronaphthalene amides (THNAs) as a new class of ATP synthase inhibitors that are effective in preventing the growth of Mycobacterium tuberculosis (M.tb) in culture. Design, synthesis and comprehensive structure-activity relationship studies for approx. 80 THNA analogs are described, with a small selection of compounds exhibiting potent (in some cases MIC90 <1 μg/mL) in vitro M.tb growth inhibition taken forward to pharmacokinetic and off-target profiling studies. Ultimately, we show that some of these THNAs possess reduced lipophilic properties, decreased hERG liability, faster mouse/human liver microsomal clearance rates and shorter plasma half-lives compared with bedaquiline, potentially addressing of the main concerns of persistence and phospholipidosis associated with bedaquiline. In the part of experimental materials, we found many familiar compounds, such as Methyl 5-bromopicolinate(cas: 29682-15-3Quality Control of Methyl 5-bromopicolinate)
Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. When pyridine is adsorbed on oxide surfaces or in porous materials, the following species are commonly observed: (i) pyridine coordinated to Lewis acid sites, (ii) pyridine H-bonded to weakly acidic hydroxyls, and (iii) protonated pyridine. At high coverage, physisorbed pyridine and protonated dimers can also be observed.Quality Control of Methyl 5-bromopicolinate