Yves Pascal | Researchain

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Featured researches published by Yves Pascal.

Bioorganic & Medicinal Chemistry Letters | 2000

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

Yves Pascal; Charles R Andrianjara; Eric Auclair; Nadine Avenel; Bernadette Bertin; Alain Calvet; Frederic Feru; Sophie Lardon; Indres Moodley; Malika Ouagued; Adrian Payne; Marie-Pierre Pruniaux; Corinne Szilagyi

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.

Journal of Medicinal Chemistry | 2000

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.

Catherine Burnouf; Eric Auclair; Nadine Avenel; Bernadette Bertin; Christèle Bigot; Alain Calvet; Kam Chan; Corinne Durand; Veronique Fasquelle; Frederic Feru; Richard B. Gilbertsen; Henry Jacobelli; Adel Kebsi; Emmanuelle Lallier; Jacquie Maignel; Brigitte Martin; Stéphane Milano; Malika Ouagued; Yves Pascal; Marie-Pierre Pruniaux; Jocelyne Puaud; Marie-Noëlle Rocher; Christophe Terrasse; and Roger Wrigglesworth; Annette Marian Doherty

Archive | 1997