20172-97-8Relevant articles and documents
Inhibitors of fumarylacetoacetate hydrolase domain containing protein 1 (Fahd1)
Eder, Manuel Philip,Gstach, Hubert,Jansen-Dürr, Pidder,Klapec, Patrycia,Liedl, Klaus R.,Loeffler, Johannes R.,Monteleone, Stefania,Weiss, Alexander K. H.,Wurzer, Richard,von Grafenstein, Susanne
, (2021/08/26)
FAH domain containing protein 1 (FAHD1) acts as oxaloacetate decarboxylase in mitochondria, contributing to the regulation of the tricarboxylic acid cycle. Guided by a high-resolution X-ray structure of FAHD1 liganded by oxalate, the enzymatic mechanism of substrate processing is analyzed in detail. Taking the chemical features of the FAHD1 substrate oxaloacetate into account, the potential inhibitor structures are deduced. The synthesis of drug-like scaffolds afforded first-generation FAHD1-inhibitors with activities in the low micromolar IC50 range. The investigations disclosed structures competing with the substrate for binding to the metal cofactor, as well as scaffolds, which may have a novel binding mode to FAHD1.
A synthesis method of grass amide derivatives (by machine translation)
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Paragraph 0017, (2017/08/28)
The present invention provides a D. amide derivatives of synthetic method. It adopts the D. amide and halogenated compound reaction, adding alkali, bidentate ligand, copper salt catalyst, solvent, the solvent reflux temperature of the reaction a certain period of time and then after treatment. The turf amide with a halo compound in a molar ratio of 1: 0.4 - 3.5; the turf amide with alkali molar ratio of 1: 1.0 - 3.0; the D. amide with the bidentate ligand molar ratio of 1:5 - 25 μM %; the turf amide with the molar ratio of the copper salt catalyst: 1:5 - 30 μM %. The process method is different from the reported oxalic acid diester or oxalyl with different amino substituted compound of method. The invention in the existing technology based on the use of a readily available and inexpensive D. as raw materials, accord with the green chemistry, to avoid colorless fuming liquid of the adding of the oxalyl, increase operability, is suitable for industrial production. (by machine translation)
Crystal structure and DNA-binding study of a monoclinic polymorph of N,N′-bis(2-pyridyl)oxamide
Zhang, Wan-Ju,Zhang, Kai,Wang, Fang
, p. 712 - 716 (2015/02/19)
A monoclinic polymorph of N,N′-bis(2-pyridyl)oxamide has been synthesized and characterized by single-crystal X-ray diffract ion method. It crystallizes in monoclinic, space group C2/c with crystallographic data: a = 10.596(3) A, b = 12.950(3) A, c = 8.612(2) A, β = 90.935(8)° and Z = 4. In the polymorph, two-dimensional network is formed by hydrogen bond and π-π stacking interact ion. The binding studies of the compound with calf thymus DNA (CT-DNA) have also been explored by elect ronic absorpt ion t it rat ion and fluorescence quenching experiments, and the results suggest that the compound binds to CT-DNA through groove binding.