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Structure-activity analysis of CJ-15,801 analogues that interact with Plasmodium falciparum pantothenate kinase and inhibit parasite proliferation

Spry, Christina; Sewell, Alan L; Hering, Yuliya; Villa, Mathew V J; Weber, Jonas; Hobson, Stephen J; Harnor, Suzannah J; Gul, Sheraz; Marquez, Rodolfo; Saliba, Kevin J

Description

Survival of the human malaria parasite Plasmodium falciparum is dependent on pantothenate (vitamin B5), a precursor of the fundamental enzyme cofactor coenzyme A. CJ-15,801, an enamide analogue of pantothenate isolated from the fungus Seimatosporium sp. CL28611, was previously shown to inhibit P. falciparum proliferation in vitro by targeting pantothenate utilization. To inform the design of next generation analogues, we set out to synthesize and test a series of synthetic enamide-bearing...[Show more]

CollectionsANU Research Publications
Date published: 2018-01-01
Type: Journal article
URI: http://hdl.handle.net/1885/139108
Source: European journal of medicinal chemistry
DOI: 10.1016/j.ejmech.2017.08.050

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