scholarly journals Design, Synthesis, and Biological Evaluation of Sphingosine 1-Phosphate Receptor (S1PR) Agonists

2014 ◽  
Author(s):  
Michael Ferracane
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Sphingosine 1 Phosphate ◽  
Synthesis And Biological Evaluation

Design, synthesis and biological evaluation as immunosuppressant of amino alcohol derivatives containing thioether

2021 ◽  
Vol 11 (5) ◽  
pp. 773-780
Author(s):  
Yanjie Li ◽  
Yongqiang Li ◽  
Liu Yang ◽  
Zhi Liu ◽  
Ruimeng Zhang ◽  
...  
Keyword(s):  
Amino Alcohol ◽  
Coupling Reaction ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Suzuki Coupling Reaction ◽  
Sphingosine 1 Phosphate ◽  
Potential Activity ◽  
Key Steps ◽  
Synthesis And Biological Evaluation

To develop a safer immunosuppressant for organ transplantation and autoimmune disease treatment, in this study, several of novel amino alcohol derivatives containing thioether moiety were synthesized with 7-bromo-tetralin-2-one as starting material, and Suzuki coupling reaction and Bucherer-Bergs reaction as key steps. Their activity as sphingosine 1-phosphate receptor type 1 (S1P1) agonists were evaluated by [γ-35S] GTP binding assay. Among the thioether substituted compounds, compound 10 showed good activity as S1P1 agonist at low micromolar concentration (EC50 = 0.698 μmol/L). The result suggested that it has potential activity against autoimmune diseases and immunosuppressant of organ transplantations.

Design, Synthesis and Biological Evaluation of Hybrid Molecules Containing Conjugated Styryl Ketone and α-Bromoacryloyl Moieties

2012 ◽  
Vol 9 (2) ◽  
pp. 140-152 ◽  
Author(s):  
Romeo Romagnoli ◽  
Pier Giovanni Baraldi ◽  
Olga Cruz-Lopez ◽  
Maria Kimatrai Salvador ◽  
Delia Preti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Hybrid Molecules ◽  
Synthesis And Biological Evaluation

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Design, Synthesis and Biological Evaluation of Benzopyran Derivatives as KATP Channel Openers

2010 ◽  
Vol 7 (6) ◽  
pp. 415-420 ◽  
Author(s):  
Jinpei Zhou ◽  
Hai Qian ◽  
Huibin Zhang ◽  
Hui Gao ◽  
Wenlong Huang ◽  
...  
Keyword(s):  
Katp Channel ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Katp Channel Openers
Sign in / Sign up

Export Citation Format

Share Document