Aminoquinoline-Pyrimidine-Based Alkyl-Piperazine Tethered Hybrids: Synthesis, Antiplasmodial Activity, and Mechanistic Studies.

ABSTRACT: Though great progress has been made to eliminate malaria globally, effective and inexpensive strategies to design new antimalarials are still required due to the problem of drug resistance to the currently used antimalarials. Herein, in continuation of our efforts to improve the therapeutic efficacy of 4-aminoquinoline-pyrimidine (4-AQ-Py) based molecular hybrids, a series of 4-AQ-Py hybrids linked through diamine-piperazine (flexible and rigid) linkers was synthesized and assessed for in vitro antiplasmodial activity. In the in vitro assay, these hybrids exhibited excellent potency and selectivity index against both the chloroquine (CQ)-sensitive (D6) and CQ-resistant (W2) strains of Plasmodium falciparum. Compound 7i was found to be the most pote

SUBMITTER: Rawat S 

PROVIDER: S-EPMC11966289 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature