126167-36-0Relevant academic research and scientific papers
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
Pascal, Yves,Andrianjara, Charles R.,Auclair, Eric,Avenel, Nadine,Bertin, Bernadette,Calvet, Alain,Feru, Frederic,Lardon, Sophie,Moodley, Indres,Ouagued, Malika,Payne, Adrian,Pruniaux, Marie-Pierre,Szilagyi, Corinne
, p. 35 - 38 (2007/10/03)
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.
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6,7,1-hi]indoles: Discovery of potent, selective phosphodiesterase type 4 inhibitors
Burnouf,Auclair,Avenel,Bertin,Bigot,Calvet,Chan,Durand,Fasquelle,Féru,Gilbertsen,Jacobelli,Kebsi,Lallier,Maignel,Martin,Milano,Ouagued,Pascal,Pruniaux,Puaud,Rocher,Terrasse,Wrigglesworth,Doherty
, p. 4850 - 4867 (2007/10/03)
The synthesis, structure-activity relationships, and biological properties of a novel series of potent and selective phosphodiesterase type 4 (PDE4) inhibitors are described. These new aminodiazepinoindoles displayed in vitro PDE4 activity with submicromo
