Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores.
Eur J Med Chem
; 131: 171-184, 2017 May 05.
Article
em En
| MEDLINE
| ID: mdl-28319782
ABSTRACT
Due to the recent reports of growing parasite resistance to artemisinins and other antimalarial drugs, development of new antimalarial chemotypes is an urgent priority. Here in, we report a novel series of adamantyl/cycloheptyl indoleamide derivatives bearing sulfonamide and triazole pharmacophores adopting different chemical modifications and evaluated them for antiplasmodial activity in vitro. Among all the indoleamides, compounds 22, 24, 26 and 30 with sulfonamide pharmacophore showed promising activity with IC50 of 1.87, 1.93, 2.00, 2.17 µM against CQ sensitive Pf3D7 strain and 1.69, 2.12, 1.60, 2.19 µM against CQ resistant PfK1 strain, respectively.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
/
Sulfanilamidas
/
Triazóis
/
Antimaláricos
Limite:
Animals
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article