Author/Authors :
Jon Wright، نويسنده , , Gary Bolton، نويسنده , , Mark Creswell، نويسنده , , Dennis Downing، نويسنده , , Lynn Georgic، نويسنده , , Thomas Heffner، نويسنده , , John Hodges، نويسنده , , A. ROBERT MACKENZIE ، نويسنده , , Lawrence Wise، نويسنده ,
Abstract :
A novel series of 8-amino-6-(arylsulphonyl)-5-nitroquinoline neuropeptide Y1 (NPY) receptor antagonists is reported. The 8-amino and 5-nitro groups were important for NPY1 binding affinity as changes caused large drops in potency. The 6-arylsulphonyl group was necessary; however, substitution on the phenyl was tolerated. The 2-isopropyl analog 21 was a moderately potent, highly selective NPY1 receptor antagonist.