1,3-Phenylene bis(ketoacid) derivatives as inhibitors of Escherichia coli dihydrodipicolinate synthase

Identification of thebona fideDHDPS from a common plant pathogen

“…With regards to the active site, a number of inhibitors based on substrate and product analogs have previously been investigated, but these exhibit only moderate (m M ) inhibition potencies . More success has been achieved with inhibitors based on the acyclic enzyme‐bound DHDPS intermediates, which irreversibly inhibit DHDPS, but most remain in the low millimolar range. However, our structural studies show that two distinct conformations of the key catalytic triad residue Tyr133 exist, which are likely to represent an active and inactive form of the enzyme.…”

Dimerization of Bacterial Diaminopimelate Epimerase Is Essential for Catalysis

“…Mass Spectrometry-Mass spectrometric analyses were performed on an Agilent 6220 Accurate-Mass TOF LC/MS mass spectrometer coupled to an Agilent 1100 LC system (Agilent, Palo Alto, CA) as described previously (23,24). Protein samples were left in their original buffer (typically 20 mM Tris, 150 mM NaCl, pH 8.0) and were loaded onto an Agilent Poroshell 300SB-C18 2.1 ϫ 75-mm, 5-m reverse phase column attached to the mass spectrometer.…”

Two-Step Continuous Synthesis of Dicarbonyl Indoles via I2/DMSO-Promoted Oxidative Coupling: A Green and Practical Approach to Valuable Diketones from Aryl Acetaldehydes

“…Indole derivatives are widespread in natural products, pharmaceutical molecules, and agrochemicals. − Owing to the excellent features, functional modification of indoles is an important research topic in organic and medicinal chemistry. − Notably, C-3 dicarbonyl indoles containing indolyl diketone scaffolds have attracted lots of interest from chemists all over the world because of not only their remarkable biological and pharmacological activities but also their wide application as precursors for various organic transformations. − Recent studies have disclosed that some dicarbonyl indole derivatives could behave as positive or negative allosteric modulators of A 2B AR and represent new pharmacological tools useful for the development of therapeutic agents to treat pathological conditions related to an altered functionality of A 2B AR. , In addition, α-ketoamides and α-ketoesters as kinds of well-known and valuable diketones have been also widely researched in organic synthesis and pharmaceutical chemistry by chemists worldwide. − Consequently, green and practical approaches to these valuable diketones from readily available starting materials are still desirable.…”