Miller, William H.; Seefeld, Mark A.; Newlander, Kenneth A.; Uzinskas, Irene N.; Burgess, Walter J.; Heerding, Dirk A.; Yuan, Catherine C. K.; Head, Martha S.; Payne, David J.; Rittenhouse, Stephen F.; Moore, Terrance D.; Pearson, Stewart C.; Berry, Valerie; DeWolf, Walter E. Jr.; Keller, Paul M.; Polizzi, Brian J.; Qiu, Xiayang; Janson, Cheryl A.; Huffman, William F. published an article in Journal of Medicinal Chemistry. The title of the article was 《Discovery of Aminopyridine-Based Inhibitors of Bacterial Enoyl-ACP Reductase (FabI)》.Name: 3-(6-Aminopyridin-3-yl)propanoic acid The author mentioned the following in the article:
Bacterial enoyl-ACP reductase (FabI) catalyzes the final step in each cycle of bacterial fatty acid biosynthesis and is an attractive target for the development of new antibacterial agents. Our efforts to identify potent, selective FabI inhibitors began with screening of the GlaxoSmithKline proprietary compound collection, which identified several small-mol. inhibitors of Staphylococcus aureus FabI. Through a combination of iterative medicinal chem. and X-ray crystal structure based design, one of these leads was developed into the novel aminopyridine derivative I, a low micromolar inhibitor of FabI from S. aureus (IC50 = 2.4 μM) and Haemophilus influenzae (IC50 = 4.2 μM). Compound I has good in vitro antibacterial activity against several organisms, including S. aureus (MIC = 0.5 μg/mL), and is effective in vivo in a S. aureus groin abscess infection model in rats. Through FabI overexpressor and macromol. synthesis studies, the mode of action of I has been confirmed to be inhibition of fatty acid biosynthesis via inhibition of FabI. Taken together, these results support FabI as a valid antibacterial target and demonstrate the potential of small-mol. FabI inhibitors for the treatment of bacterial infections.3-(6-Aminopyridin-3-yl)propanoic acid(cas: 446263-96-3Name: 3-(6-Aminopyridin-3-yl)propanoic acid) was used in this study.
3-(6-Aminopyridin-3-yl)propanoic acid(cas: 446263-96-3) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Name: 3-(6-Aminopyridin-3-yl)propanoic acid