341529-34-8Relevant articles and documents
N-Acylbenzotriazole: convenient approach for protecting group-free monoacylation of symmetric diamines
Agha, Khalid A.,Abo-Dya, Nader E.,Ibrahim, Tarek S.,Abdel-Aal, Eatedal H.,Abdel-Samii, Zakaria K.
, p. 589 - 598 (2020/05/06)
Abstract: An efficient green route for monoacylation of aromatic diamines, namely o-phenylenediamine and p-phenylenediamine and aliphatic diamines ethylenediamine and piperazine using N-acylbenzotriazoles (NABs) in n-butanol was developed. The new protocol does not require prior selective protection of the diamine and comprises simple conditions, short reaction times, an easy work up as well as high isolated yields (69–94%). Moreover, the method described herein enable stepwise acylation of aliphatic diamines such as ethylenediamine and piperazine with two different N-acylbenzotriazoles affording unsymmetrical substituted diamines that can be used for construction of pharmaceutically important targets such as drugs, foldamers, and drug conjugates. Graphic abstract: [Figure not available: see fulltext.]
Thienopyrimidinone compound and use thereof
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Paragraph 0031; 0035; 0038; 0046; 0047, (2019/01/20)
The invention belongs to the field of chemical medicines and specifically relates to a thienopyrimidinone compound. The thienopyrimidinone compound has a structural formula shown in the description. The novel thienopyrimidinone compound can produce good inhibition effects on Tankyrase, has no obvious toxicity, can obviously inhibit the proliferation of tumor cells after STF3A cell treatment basedon the compound, has the good medicinal potential and provides a novel potential choice for clinical medication. The novel thienopyrimidinone compound can improve the expression level of an axin in the wnt signal pathway, induce the degradation of beta-catenin, thereby inhibiting the proliferation of tumor cells, can be used as a clinical prodrug candidate compound for various tumor cells and hasfurther research and development potential. A preparation method of the thienopyrimidinone compound can produce the compound with a high yield and high biological activity. The thienopyrimidinone compound has significant drug properties and has broad market prospects.
Synthesis, characterization, and anti-inflammatory activities of methyl salicylate derivatives bearing piperazine moiety
Li, Jingfen,Yin, Yong,Wang, Lisheng,Liang, Pengyun,Li, Menghua,Liu, Xu,Wu, Lichuan,Yang, Hua
, (2016/12/02)
In this study, a new series of 16 methyl salicylate derivatives bearing a piperazine moiety were synthesized and characterized. The in vivo anti-inflammatory activities of target compounds were investigated against xylol-induced ear edema and carrageenan-induced paw edema in mice. The results showed that all synthesized compounds exhibited potent anti-inflammatory activities. Especially, the anti-inflammatory activities of compounds M15 and M16 were higher than that of aspirin and even equal to that of indomethacin at the same dose. In addition, the in vitro cytotoxicity activities and anti-inflammatory activities of four target compounds were performed in RAW264.7 macrophages, and compound M16 was found to significantly inhibit the release of lipopolysaccharide (LPS)-induced interleukin (IL)-6 and tumor necrosis factor (TNF)-α in a dose-dependent manner. In addition, compound M16 was found to attenuate LPS induced cyclooxygenase (COX)-2 up-regulation. The current preliminary study may provide information for the development of new and safe anti-inflammatory agents.