22362-66-9Relevant articles and documents
OXADIAZOLE AND PHENOL DERIVATIVES AS ANTIBACTERIAL AND/OR HERBICIDAL AGENTS
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Paragraph 0221; 0222, (2018/10/19)
Antimicrobial resistance is rising at an alarming rate. The methylerythritol phosphate (MEP) pathway is a metabolic pathway that produces the isoprenoids isopentyl pyrophosphate (IPP) and dimethylallyl pyrophosphate (DMAPP). Notably, the MEP pathway is present in bacteria and not mammals, which made the enzymes of the MEP pathway attractive targets for discovering new anti-infective agents due to reduced chances of off-target interactions leading to side effects. The biophysical properties of 2-C-methyl-D-erythritol 4-phosphate cytidylyltransferase (IspD) and 4-diphosphocytidyl-2-C-methyl-D-erythritol kinase (IspE) were determined to aid discovery of novel inhibitors. Thermal shift screening was used as an initial filter to narrow down a library of compounds with thermal shifts greater than 1° C., which could indicate binding to the IspD and IspE enzymes. Follow-up studies were performed using isothermal titration calorimetry and enzymatic inhibition assays. Results from these studies have revealed compounds with high micromolar inhibition of both IspD from Escherichia coli and IspE from Burkholderia thailandensis. The hit compounds are used for future development of more potent IspD and IspE inhibitors.
synthesis of some 4-methyl-2-(3-methylbenzofuran-2- yl)quinoline -3-carboxylic acids
Fu, Xin B.,Li, Yang,Gao, Wen T.
, p. 87 - 93 (2019/01/18)
In the present investigation, one-pot synthetic route for the synthesis of 4-methyl-2-(3- methylbenzofuran-2-yl)quinoline-3-carboxylic acids 3a-f has been described, involving the reaction of ethyl 2- (chloromethyl)-4-methylquinoline-3-carboxylate (1) with various 1-(2-hydroxyphenyl)ethanones 2a-f in refluxing MeCN with the presence of K2 CO3 as base and PEG-400 as phase transfer catalyst. The structures of all the newly- 2 3 synthesized compounds were confirmed by IR, 1H NMR, 13C NMR and HRMS.
Cu-Mn spinel oxide catalyzed regioselective halogenation of phenols and N-heteroarenes
Singh, Parvinder Pal,Thatikonda, Thanusha,Kumar, K. A. Aravinda,Sawant, Sanghapal D.,Singh, Baldev,Sharma, Amit Kumar,Sharma,Singh, Deepika,Vishwakarma, Ram A.
experimental part, p. 5823 - 5828 (2012/09/05)
A novel simple, mild chemo- and regioselective method has been developed for the halogenation of phenols using Cu-Mn spinel oxide as a catalyst and N-halosuccinimide as halogenating agent. In the presence of Cu-Mn spinel oxide B, both electron-withdrawing and electron-donating groups bearing phenols gave monohalogenated products in good to excellent yields with highest para-selectivity. The para-substituted phenol gave monohalogenated product with good yield and ortho-selectivity. N-Heteroarenes such as indoles and imidazoles also gave monohalogenated products with high selectivity. Unlike the copper-catalyzed halogenation, the present method works well with electron-withdrawing group bearing phenols and gives comparatively better yields and selectivity. The Cu-Mn spinel catalyst is robust and reused three times under optimized conditions without any loss in catalytic activity. Nonphenolics did not undergo this transformation.
