Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides
Braz. J. Pharm. Sci. (Online)
; 53(1): e16067, 2017. tab, graf
Article
in English
| LILACS
| ID: biblio-839450
Responsible library:
BR1.1
ABSTRACT
ABSTRACT We describe herein the synthesis and evaluation of the antileishmanial activity against promastigote forms of Leishmania amazonensis and cytotoxicity to murine macrophages of a series of 2-chloro-N-arylacetamide derivatives. All compounds were active, except one (compound 3). Compound 5 presented the most promising results, showing good antileishmanial activity (CI50=5.39±0.67 µM) and moderate selectivity (SI=6.36), indicating that further development of this class is worthwhile. Preliminary QSAR studies, although not predictive, furnished some insights on the importance of electronic character of aryl substituent to biological activity, as well as an indirect influence of hydrophobicity on activity.
Full text:
Available
Collection:
International databases
Database:
LILACS
Main subject:
Leishmaniasis
/
Quantitative Structure-Activity Relationship
Type of study:
Prognostic study
Limits:
Animals
Language:
English
Journal:
Braz. J. Pharm. Sci. (Online)
Journal subject:
Farmacologia
/
Teraputica
/
Toxicologia
Year:
2017
Document type:
Article
Affiliation country:
Brazil
Institution/Affiliation country:
Universidade Federal de Minas Gerais/BR