Title of article :
Potent, selective, and orally active adenosine A2A receptor antagonists: Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines
Author/Authors :
Bernard R. Neustadt، نويسنده , , Jinsong Hao، نويسنده , , Neil Lindo، نويسنده , , William J. Greenlee، نويسنده , , Andrew W. Stamford، نويسنده , , Deen Tulshian، نويسنده , , Ennio Ongini، نويسنده , , John Hunter، نويسنده , , Angela Monopoli، نويسنده , , Rosalia Bertorelli، نويسنده , , Carolyn Foster، نويسنده , , Leyla Arik، نويسنده , , Jean Lachowicz، نويسنده , , Kwokei Ng، نويسنده , , Kung-I Feng، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2007
Abstract :
Antagonism of the adenosine A2A receptor offers great promise in the treatment of Parkinson’s disease. Employing the known pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A2A antagonist SCH 58261 as a starting point, we identified the potent and selective (vs. A1) antagonist 11 h, orally active in the rat haloperidol-induced catalepsy model. We further optimized this lead to the methoxyethoxyethyl ether 12a (SCH 420814), which shows broad selectivity, good pharmacokinetic properties, and excellent in vivo activity.
Keywords :
Parkinson’s , Adenosine A2A , 3-e]-1 , 5-c]pyrimidine , 2 , catalepsy
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
