Synthesis and evaluation of phenoxyoxazaphospholidine, phenoxyoxazaphosphinane, and benzodioxaphosphininamine sulfides and related compounds as potential anti-malarial agents
Citation:
Mara C, Dempsey E, Bell A & Barlow JW, Synthesis and evaluation of phenoxyoxazaphospholidine, phenoxyoxazaphosphinane, and benzodioxaphosphininamine sulfides and related compounds as potential anti-malarial agents, Bioorganic & Medicinal Chemistry Letters, 23, 2013, 3580 - 3583Download Item:
Abstract:
A series of phenoxyoxazaphospholidine, phenoxyoxazaphosphinane and benzodioxaphosphininamine sulfides and related cyclic organophosphorus compounds based on the lead anti-tubulin herbicides amiprophos methyl and butamifos were synthesised and evaluated for anti-malarial activity. Of these compounds, while none of the phenoxyoxazaphospholidines, phenoxyoxazaphosphinanes or benzodioxaphosphininamine sulphides were more potent than APM, phosphorothioamidate 30, a dual compound also bearing an aminoquinoline motif, showed promising activity against Plasmodium falciparum (IC50 0.038 ?M) and warrants further study.
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Enterprise Ireland
PC/2005/070
Author's Homepage:
http://people.tcd.ie/abellhttp://people.tcd.ie/dempseen
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PUBLISHED
Author: BELL, ANGUS; DEMPSEY, ENDA
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Bioorganic & Medicinal Chemistry Letters;23;
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