Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.
The synthesis and SAR studies of spiroquinazolinones as novel PDE7 inhibitors are discussed. The best compounds from the series displayed nanomolar inhibitory affinity and were selective versus other PDE isoenzymes.
Pfizer Global Research and Development, 3-9 rue de la Loge 94265 Fresnes, France. edwige.lorthois@pharma.novartis.com
Edwige
E
Lorthiois
Patrick
P
Bernardelli
Fabrice
F
Vergne
Chrystelle
C
Oliveira
Abdel-Kader
AK
Mafroud
Emmanuelle
E
Proust
Lamia
L
Heuze
François
F
Moreau
Moulay
M
Idrissi
Anita
A
Tertre
Bernadette
B
Bertin
Magali
M
Coupe
Roger
R
Wrigglesworth
Arnaud
A
Descours
Patricia
P
Soulard
Patrick
P
Berna
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002460:Cell Line; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D012995:Solubility; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D007527:Isoenzymes; D010726:Phosphodiesterase Inhibitors; D011799:Quinazolines; D013141:Spiro Compounds; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7