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
Mefenpyr-diethyl impurity, preparation method and applications thereof
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Paragraph 0024-0026, (2020/02/14)
The invention discloses a mefenpyr-diethyl impurity, a preparation method and applications thereof, wherein the molecular structural formula is represented by a formula I. The preparation method comprises: carrying out diazotization and a Japp-Klingemann reaction by using 2,4,-dichloroaniline, nitrite and ethyl 2-chloroacetoacetate as raw materials to obtain an intermediate, and carrying out a ring-closure reaction on the intermediate and ethyl methacrylate to obtain 1,5-bis(2,4-dichlorophenyl)-6-methyl-1H,5H-pyrazolo[5,1-c]-1,2,4-triazole-3,6,7a-triethyl tricarboxylate, wherein the yield reaches more than 40%. According to the invention, the method has advantages of mild reaction conditions, low energy consumption, high economic feasibility and high yield; and the substance has the application value in the influence on the efficacy of mefenpyr-diethyl by using the substance as the impurity and in the safety evaluation of the residual substance on agricultural products.