Discovery of a potent, metabolically stabilized resorcylic lactone as an anti-inflammatory lead.
Bioorg Med Chem Lett
; 19(21): 6196-9, 2009 Nov 01.
Article
in En
| MEDLINE
| ID: mdl-19783437
ABSTRACT
With bioactivity-guided phenotype screenings, a potent anti-inflammatory compound f152A1 has been isolated, characterized and identified as the known natural product LL-Z1640-2. Metabolic instability precluded its use for the study on animal disease models. Via total synthesis, a potent, metabolically stabilized analog ER-803064 has been created; addition of the (S)-Me group at C4 onto f152A1 has resulted in a dramatic improvement on its metabolic stability, while preserving the anti-inflammatory activities.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Lactones
/
Anti-Inflammatory Agents
Type of study:
Prognostic_studies
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2009
Document type:
Article
Affiliation country:
United States