Synthesis, antimalarial activity and molecular docking of hybrid 4-aminoquinoline-1,3,5-triazine derivatives.

Abstract:

:A series of novel hybrid 4-aminoquinoline 1,3,5-triazine derivatives was synthesized in a five-steps reaction and evaluated for their in vitro antimalarial activity against chloroquine-sensitive (3D7) and chloroquine-resistant (RKL-2) strains of Plasmodium falciparum. Entire synthetic derivatives showed higher antimalarial activity on the sensitive strain while two compounds, viz., 9a and 9c displayed good activity against both the strains of P. falciparum. The observed activity was further substantiated by docking study on both wild and qradruple mutant type P. falciparum dihydrofolate reductase-thymidylate synthase (pf-DHFR-TS).

journal_name

Exp Parasitol

authors

Bhat HR,Singh UP,Thakur A,Kumar Ghosh S,Gogoi K,Prakash A,Singh RK

doi

10.1016/j.exppara.2015.06.016

subject

Has Abstract

pub_date

2015-10-01 00:00:00

pages

59-67

eissn

0014-4894

issn

1090-2449

pii

S0014-4894(15)30006-0

journal_volume

157

pub_type

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