Author/Authors :
Kevin W. Moore، نويسنده , , Katrine Bonner، نويسنده , , Elizabeth A. Jones، نويسنده , , Frances Emms، نويسنده , , Paul D. Leeson، نويسنده , , Rosemary Marwood، نويسنده , , Shil Patel، نويسنده , , Smita Patel، نويسنده , , Michael Rowley، نويسنده , , P. Steven Thomas، نويسنده , , Robert W Carling، نويسنده ,
Abstract :
The syntheses of a number of different N-linked heterocyclic pyrazole replacements based on the structure 1 are described (compounds 3–12) as hD4 ligands. After further optimisation the best compound identified was 13 which has high affinity for hD4 (5.2 nM) and>300-fold selectivily for hD4 receptors over hD2 and hD3 receptors.
