An amidation/cyclization approach to the synthesis of N-hydroxyquinolinones and their biological evaluation as potential anti-plasmodial, anti-bacterial, and iron(II)-chelating agents.
Bioorg Med Chem Lett
; 25(3): 607-10, 2015 Feb 01.
Article
in En
| MEDLINE
| ID: mdl-25544370
ABSTRACT
A 26-member library of novel N-hydroxyquinolinone derivatives was synthesized by a one-pot Buchwald-type palladium catalyzed amidation and condensation sequence. The design of these rare scaffolds was inspired from N-hydroxypyridones and 2-quinolinones classes of compounds which have been shown to have rich biological activities. The synthesized compounds were evaluated for their anti-plasmodial and anti-bacterial properties. In addition, these compounds were screened for their iron(II)-chelation properties. Notably, four of these compounds exhibited anti-plasmodial activities comparable to that of the natural product cordypyridone B.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Ferrous Compounds
/
Chelating Agents
/
Quinolones
/
Amides
/
Anti-Bacterial Agents
/
Antimalarials
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2015
Type:
Article
Affiliation country:
Singapore