Author/Authors :
Jinlong Jiang، نويسنده , , Peter Lin، نويسنده , , Myle Hoang، نويسنده , , Lehua Chang، نويسنده , , Carina Tan، نويسنده , , Scott Feighner، نويسنده , , Oksana C. Palyha، نويسنده , , Donna L. Hreniuk، نويسنده , , Jie Pan، نويسنده , , Andreas W. Sailer، نويسنده , , Nancy R. Morin، نويسنده , , Douglas J. MacNeil، نويسنده , , Andrew D. Howard، نويسنده , , Lex H.T. Van der Ploeg، نويسنده , , Mark T. Goulet، نويسنده , , Robert J. DeVita، نويسنده ,
Abstract :
Structure–activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated.
Keywords :
obesity , Antagonist , Anxiety , Quinoline , Melanin-concentrating hormone , MCH , depression
