| Title : Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase - Muscia_2014_Bioorg.Med.Chem.Lett_24_1545 |
| Author(s) : Muscia GC , Hautmann S , Buldain GY , Asis SE , Gutschow M |
| Ref : Bioorganic & Medicinal Chemistry Lett , 24 :1545 , 2014 |
|
Abstract :
A series of 2-(substituted) phenyl and 2-indolyl quinoline derivatives (10a-l) was synthesized by an efficient microwave-assisted, trifluoroacetic acid-catalyzed, solvent-free method. Evaluation of the inhibitory activity led to the identification of two quinoline inhibitors of cholesterol esterase. 2-(1H-Indol-3-yl)-6-nitro-4-phenylquinoline (10l; IC50=1.98muM) was characterized as a mixed-type inhibitor with a pronounced competitive binding mode. |
| PubMedSearch : Muscia_2014_Bioorg.Med.Chem.Lett_24_1545 |
| PubMedID: 24556381 |
| Inhibitor | CHEMBL3125351 CHEMBL3125346 |
Muscia GC, Hautmann S, Buldain GY, Asis SE, Gutschow M (2014)
Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase
Bioorganic & Medicinal Chemistry Lett
24 :1545
Muscia GC, Hautmann S, Buldain GY, Asis SE, Gutschow M (2014)
Bioorganic & Medicinal Chemistry Lett
24 :1545