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.
Lorthiois
Edwige
E
Pfizer Global Research and Development, 3-9 rue de la Loge 94265 Fresnes, France. edwige.lorthois@pharma.novartis.com
Bernardelli
Patrick
P
Vergne
Fabrice
F
Oliveira
Chrystelle
C
Mafroud
Abdel-Kader
AK
Proust
Emmanuelle
E
Heuze
Lamia
L
Moreau
François
F
Idrissi
Moulay
M
Tertre
Anita
A
Bertin
Bernadette
B
Coupe
Magali
M
Wrigglesworth
Roger
R
Descours
Arnaud
A
Soulard
Patricia
P
Berna
Patrick
P
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