Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores

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...

Full description

Saved in:
Bibliographic Details
Published in:European journal of medicinal chemistry 2017-05, Vol.131, p.171-184
Main Authors: Devender, N., Gunjan, Sarika, Tripathi, Renu, Tripathi, Rama Pati
Format: Article
Language:English
Subjects:
Animals
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Antiplasmodial activity
Cercopithecus aethiops
Dose-Response Relationship, Drug
Indoleamide
Indoles - chemical synthesis
Indoles - chemistry
Indoles - pharmacology
Molecular Structure
Parasitic Sensitivity Tests
Plasmodium falciparum - drug effects
Structure-Activity Relationship
Sulfanilamides - chemistry
Sulfanilamides - pharmacology
Sulfonamide
Triazole
Triazoles - chemistry
Triazoles - pharmacology
Vero Cells
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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. [Display omitted] •Indoleamides bearing sulfonamide and triazole pharmacophores were synthesised.•Total fifty three novel compounds were synthesised.•Four compounds have shown antiplasmodial activity with IC50 of 1.60–2.19 µM.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2017.03.010