27143-12-0Relevant articles and documents
4-Cyano-5-(2-thiophenyl)-pyrazoles are high affinity CB1 receptor ligands
Altomonte, Stefano,Baillie, Gemma L.,Ross, Ruth A.,Zanda, Matteo
, p. 13692 - 13701 (2015)
Pyrazoles bearing a 5-thiophenyl and a 4-cyano group were synthesised and tested for their affinity to the cannabinoid CB1 receptor showing in many cases single digit nanomolar Ki values and moderate to good selectivity towards the CB2 receptor. Some of these pyrazole ligands, such as 8g, displayed relatively low lipophilicity (experimental logP 90) suggesting that these compounds may behave as peripherally restricted CB1 ligands. Furthermore, 2-fluoroethyl carboxamides 8d, 8h and 8l are interesting candidates for further development into PET tracers. This journal is
Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists
Chu, Bizhu,Jiang, Yuyang,Li, Qinyuan,Liu, Zijian,Luo, Jingyi,Shi, Zhichao,Xin, Qilei,Ye, Lizhen,Zhan, Feng,Zhang, Xun,Zhu, Qingyun
, (2021/09/20)
Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid–leucine–arginine sequence-contained chemokines CXCs (ELR+ CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block
Preparation method of mefenpyr-diethyl
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Paragraph 0047-0049, (2020/09/09)
The invention relates to a preparation method of mefenpyr-diethyl, which specifically comprises the following steps: (a) mixing ethyl 2-chloroacetoacetate, 2,4-dichloroaniline, inorganic acid and water, and then adding a sodium nitrite aqueous solution to form a reaction system, and performing diazotization and substitution reactions, so as to obtain ethyl 2-chloro-2-(2,4-dichlorobenzene diazo) acetoacetate; and (b) adding an inorganic base into the reaction system to adjust the pH value to 5-7, then adding a bicarbonate aqueous solution to carry out a hydrolysis reaction to obtain ethyl 2-chloro-2-(2,4-dichlorobenzylidenehydrazino)acetate, then sequentially adding a polymerization inhibitor, ethyl methacrylate and the bicarbonate aqueous solution to carry out cyclization, and carrying outpost-treatment to obtain the mefenpyr-diethyl. Compared with the prior art, the intermediate generated through diazotization and substitution is stable, the intermediate does not need to be separated, the method is easy and convenient to operate, reaction conditions are mild, sodium bicarbonate (or potassium bicarbonate) is used for hydrolysis, the raw material price is low, and the dosage is small.