60277-22-7Relevant articles and documents
THIAZOLOPIPERAZINE DERIVATIVES AND COMPOSITION FOR PREVENTING OR TREATING AUTOIMMUNE DISEASES COMPRISING THE SAME
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Paragraph 0118-0126, (2020/04/01)
The present invention provides a thiazolopiperazine derivative, and a pharmaceutical composition and a health functional food composition for preventing or treating autoimmune diseases containing the same as an active component. A compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof according to the present invention can have an effect of inhibiting lysophosphatidic acid 1 (LPA1) receptor activation, thereby being able to be usefully used as the pharmaceutical composition or the health functional food composition for preventing or treating LPA1-related diseases. In addition, it is possible to effectively prevent or treat not only autoimmune diseases, but also other immune-related diseases with similar mechanisms of occurrence by using the pharmaceutical composition and the health functional food composition.COPYRIGHT KIPO 2020
Visible-Light-Driven External-Reductant-Free Cross-Electrophile Couplings of Tetraalkyl Ammonium Salts
Liao, Li-Li,Cao, Guang-Mei,Ye, Jian-Heng,Sun, Guo-Quan,Zhou, Wen-Jun,Gui, Yong-Yuan,Yan, Si-Shun,Shen, Guo,Yu, Da-Gang
, p. 17338 - 17342 (2019/01/04)
Cross-electrophile couplings between two electrophiles are powerful and economic methods to generate C-C bonds in the presence of stoichiometric external reductants. Herein, we report a novel strategy to realize the first external-reductant-free cross-electrophile coupling via visible-light photoredox catalysis. A variety of tetraalkyl ammonium salts, bearing primary, secondary, and tertiary C-N bonds, undergo selective couplings with aldehydes/ketone and CO2. Notably, the in situ generated byproduct, trimethylamine, is efficiently utilized as the electron donor. Moreover, this protocol exhibits mild reaction conditions, low catalyst loading, broad substrate scope, good functional group tolerance, and facile scalability. Mechanistic studies indicate that benzyl radicals and anions might be generated as the key intermediates via photocatalysis, providing a new direction for cross-electrophile couplings.
SAR Studies on tetrahydroisoquinoline derivatives: The role of flexibility and bioisosterism to raise potency and selectivity toward P-glycoprotein
Capparelli, Elena,Zinzi, Laura,Cantore, Mariangela,Contino, Marialessandra,Perrone, Maria Grazia,Luurtsema, Gert,Berardi, Francesco,Perrone, Roberto,Colabufo, Nicola A.
, p. 9983 - 9994 (2015/02/05)
The development of P-glycoprotein (P-gp) ligands remains of considerable interest, mostly for investigating the proteins structure and transport mechanism. In recent years, many different generations of ligands have been tested for their ability to modulate P-gp activity. The aim of the present work is to perform SAR studies on tetrahydroisoquinoline derivatives in order to design potent and selective P-gp ligands. For this purpose, the effect of bioisosteric replacement and the role of flexibility have been investigated, and four series of tetrahydroisoquinoline ligands have been developed: (a) 2-aryloxazole bioisosteres, (b) elongated analogues, (c) 2H-chromene, and (d) 2-biphenyl derivatives. The results showed that both 2-biphenyl derivative 20b and elongated derivative 6g behaved as strong P-gp substrates. In conclusion, important aspects for developing potent and selective P-gp ligands have been highlighted, providing a solid starting point for further optimization.