582-33-2Relevant articles and documents
Pleuromutilin derivative with 1, 3, 4-oxadiazole side chain and preparation and application thereof
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Paragraph 0055-0056; 0070; 0090; 0092; 0095; 0103, (2021/07/24)
The invention belongs to the field of medicinal chemistry, and particularly relates to a pleuromutilin derivative with a 1, 3, 4-oxadiazole side chain and preparation and application thereof The pleuromutilin derivative with the 1, 3, 4-oxadiazole side chain is a compound shown in a formula 2 or a pharmaceutically acceptable salt thereof, and a solvent compound, an enantiomer, a diastereoisomer and a tautomer of the compound shown in the formula 2 or the pharmaceutically acceptable salt thereof or a mixture of the solvent compound, the enantiomer, the diastereoisomer and the tautomer in any proportion, including a racemic mixture. The pleuromutilin derivative has good antibacterial activity, is especially suitable for being used as a novel antibacterial agent for systemic system infection of animals or human beings, and has good water solubility.
The discovery of novel small molecule allosteric activators of aldehyde dehydrogenase 2
Tian, Wei,Guo, Jiapeng,Zhang, Qingsen,Fang, Shaoyu,Zhou, Ruolan,Hu, Jian,Wang, Mingping,Zhang, Yuefan,Guo, Jin-Min,Chen, Zhuo,Zhu, Ju,Zheng, Canhui
, (2020/12/30)
Aldehyde dehydrogenase 2 (ALDH2) plays important role in ethanol metabolism, and also serves as an important shield from the damage occurring under oxidative stress. A special inactive variant was found carried by 35–45% of East Asians. The variant carriers have recently been found at the higher risk for the diseases related to the damage occurring under oxidative stress, such as cardiovascular and cerebrovascular diseases. As a result, ALDH2 activators may potentially serve as a new class of therapeutics. Herein, N-benzylanilines were found as novel allosteric activators of ALDH2 by computational virtual screening using ligand-based and structure-based screening parallel screening strategy. Then a structural optimization was performed and has led to the discovery of the compound C6. It has good activity in vitro and in vivo, which could reduce infarct size by ~70% in ischemic stroke rat models. This study provided good lead compounds for the further development of ALDH2 activators.
Production process of ethyl m-aminobenzoate
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Paragraph 0026-0045, (2021/04/21)
The invention provides a production process of ethyl m-aminobenzoate, and the production process comprises the following steps: filling a trickle bed reactor with a catalyst DCyPP.Pd(OAc)2 and potassium carbonate, adding a mixture of 3-chloroaniline and ethanol, introducing carbon monoxide, keeping the pressure in the reactor at 0.1-0.2 MPa, carrying out carbonylation esterification reaction, and performing purifying by a rectifying tower to obtain the ethyl m-aminobenzoate with the molar yield of 97%, wherein the purity of the ethyl m-aminobenzoate is more than 98.5%. According to the method, ethyl m-aminobenzoate can be continuously produced, reaction raw materials are convenient and easy to obtain, the process is simple, reaction conditions are mild, reaction energy consumption is low, no waste acid is generated in the reaction process, and the method is suitable for large-scale production.