From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.
Animals
Blood Proteins
/ chemistry
Celecoxib
/ chemistry
Cyclic Nucleotide Phosphodiesterases, Type 5
/ chemistry
Drug Design
Female
Half-Life
Humans
Isoenzymes
/ antagonists & inhibitors
Mice
Mice, Inbred C57BL
Microsomes, Liver
/ metabolism
Phosphodiesterase 5 Inhibitors
/ chemistry
Protein Binding
Pyrazoles
/ chemistry
Recombinant Proteins
/ biosynthesis
Stereoisomerism
Structure-Activity Relationship
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
22 04 2021
22 04 2021
Historique:
pubmed:
2
4
2021
medline:
17
6
2021
entrez:
1
4
2021
Statut:
ppublish
Résumé
A ligand-based approach involving systematic modifications of a trisubstituted pyrazoline scaffold derived from the COX2 inhibitor, celecoxib, was used to develop novel PDE5 inhibitors. Novel pyrazolines were identified with potent PDE5 inhibitory activity lacking COX2 inhibitory activity. Compound
Identifiants
pubmed: 33793216
doi: 10.1021/acs.jmedchem.0c01120
doi:
Substances chimiques
Blood Proteins
0
Isoenzymes
0
Phosphodiesterase 5 Inhibitors
0
Pyrazoles
0
Recombinant Proteins
0
Cyclic Nucleotide Phosphodiesterases, Type 5
EC 3.1.4.35
Celecoxib
JCX84Q7J1L
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM