Lead Optimization of Phthalazinone Phosphodiesterase Inhibitors as Novel Antitrypanosomal Compounds.
Animals
Crystallography, X-Ray
Drug Stability
Humans
Mice
Microsomes, Liver
/ metabolism
Molecular Structure
Parasitic Sensitivity Tests
Phosphodiesterase Inhibitors
/ chemical synthesis
Phosphoric Diester Hydrolases
/ metabolism
Phthalazines
/ chemical synthesis
Protein Binding
Protozoan Proteins
/ metabolism
Structure-Activity Relationship
Trypanocidal Agents
/ chemical synthesis
Trypanosoma brucei brucei
/ drug effects
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:
09 04 2020
09 04 2020
Historique:
pubmed:
21
3
2020
medline:
8
10
2020
entrez:
21
3
2020
Statut:
ppublish
Résumé
Human African trypanosomiasis is causing thousands of deaths every year in the rural areas of Africa. In this manuscript we describe the optimization of a family of phtalazinone derivatives. Phosphodiesterases have emerged as attractive molecular targets for a novel treatment for a variety of neglected parasitic diseases. Compound
Identifiants
pubmed: 32196340
doi: 10.1021/acs.jmedchem.9b00985
doi:
Substances chimiques
Phosphodiesterase Inhibitors
0
Phthalazines
0
Protozoan Proteins
0
Trypanocidal Agents
0
Phosphoric Diester Hydrolases
EC 3.1.4.-
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM