Synthesis, Antimalarial Activity, and Structure–Activity Relationship of 7-(2-Phenoxyethoxy)-4(1H)-quinolones | Zendy

R. Matthew Cross | Zendy; Niranjan K. Namelikonda | Zendy; Tina Mutka | Zendy; Lisa Luong | Zendy; Dennis E. Kyle | Zendy; Roman Manetsch | Zendy

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Synthesis, Antimalarial Activity, and Structure–Activity Relationship of 7-(2-Phenoxyethoxy)-4(1H)-quinolones

Author(s) -

R. Matthew Cross,

Niranjan K. Namelikonda,

Tina Mutka,

Lisa Luong,

Dennis E. Kyle,

Roman Manetsch

Publication year - 2011

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm200718m

Subject(s) - chemistry , quinolone , plasmodium berghei , atovaquone , stereochemistry , structure–activity relationship , pharmacology , ed50 , malaria , chemical synthesis , plasmodium falciparum , in vitro , biochemistry , antibiotics , immunology , biology

ICI 56,780 (5) displayed causal prophylactic and blood schizonticidal activity (ED50=0.05 mg/kg) in rodent malaria models but produced rapid acquisition of parasitological resistance in P. berghei infected mice. Herein we describe the synthesis of analogues of 5 with EC50 as low as 0.15 nM against multidrug resistant P. falciparum. Optimal activity with low cross-resistance indexes (RI) to atovaquone was achieved by introducing ortho-substituted aryl moieties at the 3-position of the 7-(2-phenoxyethoxy)-4(1H)-quinolone core.

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