Chen, Guo-Ying published the artcileApplication of Fragment-Based Drug Discovery against DNA Gyrase B, SDS of cas: 23351-09-9, the publication is ChemPlusChem (2015), 80(8), 1250-1254, database is CAplus and MEDLINE.
Bacterial resistance to antibiotics remains a serious threat to global health. The gyrase B enzyme is a well-validated target for developing antibacterial drugs. Despite being an attractive target for antibiotic development, there are currently no gyrase B inhibitory drugs on the market. A fragment screen using 1,800 compounds identified 14 fragments that bind to Escherichia coli (E. coli) gyrase B. The detailed characterization of binding is described for all 14 fragments. With the aid of X-ray crystallog., modifications on a low-affinity fragment (KD=253 μΜ, IC50=634 μΜ) has led to the development of a new class of potent Ph aminopyrazole inhibitors against E. coli gyrase B (IC50=160 nΜ). The study presented here combines the use of a set of biophys. techniques including differential scanning fluorimetry, NMR, isothermal titration calorimetry, and X-ray crystallog. to methodically identify, quantify, and optimize fragments into new chem. leads.
ChemPlusChem published new progress about 23351-09-9. 23351-09-9 belongs to alcohols-buliding-blocks, auxiliary class Pyrrole,Benzene,Alcohol, name is 4-(1H-Pyrrol-1-yl)phenol, and the molecular formula is C10H9NO, SDS of cas: 23351-09-9.
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