One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Formula: C10H7BrO2S, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 360575-29-7, Name is Methyl 4-bromobenzo[b]thiophene-2-carboxylate, molecular formula is C10H7BrO2S
Structure-based design of potent and ligand-efficient inhibitors of CTX-M class A beta-lactamase
The emergence of CTX-M class A extended-spectrum beta-lactamases poses a serious health threat to the public. We have applied structure-based design to improve the potency of a novel noncovalent tetrazole-containing CTX-M inhibitor (Ki = 21 muM) more than 200-fold via structural modifications targeting two binding hot spots, a hydrophobic shelf formed by Pro167 and a polar site anchored by Asp240. Functional groups contacting each binding hot spot independently in initial designs were later combined to produce analogues with submicromolar potencies, including 6-trifluoromethyl-3H-benzoimidazole-4- carboxylic acid [3-(1H-tetrazol-5-yl)-phenyl]-amide, which had a Ki value of 89 nM and reduced the MIC of cefotaxime by 64-fold in CTX-M-9 expressing Escherichia coli. The in vitro potency gains were accompanied by improvements in ligand efficiency (from 0.30 to 0.39) and LipE (from 1.37 to 3.86). These new analogues represent the first nM-affinity noncovalent inhibitors of a class A beta-lactamase. Their complex crystal structures provide valuable information about ligand binding for future inhibitor design.
One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Formula: C10H7BrO2S, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 360575-29-7
Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem