Author/Authors :
Shu-Hai Zhao، نويسنده , , Jacob Berger، نويسنده , , Robin D. Clark، نويسنده , , Steven G. Sethofer، نويسنده , , Nancy E. Krauss، نويسنده , , Julie M. Brothers، نويسنده , , Renee S. Martin، نويسنده , , Dinah L. Misner، نويسنده , , Dietmar Schwab، نويسنده , , Ludmila Alexandrova، نويسنده ,
Abstract :
A series of novel 3,4-dihydro-2H-benzo[1,4]oxazine derivatives has been designed and synthesized as 5-HT6 receptor antagonists. Many of the compounds displayed subnanomolar affinities for the 5-HT6 receptor and good brain penetration in rats. The relationship of structure and lipophilicity to hERG inhibition of this series of compounds is discussed.
Keywords :
5-HT6 antagonist , Benzoxazine , HERG , Lipophilicity , Brain penetration
