Title of article :
Synthesis and structure–activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors
Author/Authors :
Yves Pascal، نويسنده , , Charles R. Andrianjara، نويسنده , , Eric Auclair، نويسنده , , Nadine Avenel، نويسنده , , Bernadette Bertin، نويسنده , , Alain Calvet، نويسنده , , Frédéric Féru، نويسنده , , Sophie Lardon، نويسنده , , Indres Moodley، نويسنده , , Malika Ouagued، نويسنده , , Adrian Payne، نويسنده , , Marie-Pierre Pruniaux، نويسنده , , Corinne Szilagyi، نويسنده ,
Abstract :
A novel series of benzodiazepine derivatives have been discovered as inhibitors of PDE4 enzymes. We have found that our compounds are selective versus other PDE enzymes, and that the activity can be modulated by specific structural modifications. One compound exhibited a strong eosinophilic infiltration inhibiting action on sensitized Brown-Norway rats (compound 9, 5.1 mg/kg p.o.), moreover this compound is not emetic at 3 mg/kg i.v.
