Literature DB >> 9622557

Antimalarial cyclic peroxy ketals.

G H Posner1, H O'Dowd, P Ploypradith, J N Cumming, S Xie, T A Shapiro.   

Abstract

Over 20 new, cyclic, peroxy ketals have been prepared via a two-step protocol starting with readily available aryl methyl ketones. Structure-activity correlations using in vitro antimalarial data as a guide for optimization of potency have led to the design and synthesis of seven new peroxides that have IC50 values of 31-85 nM (artemisinin IC50 = 8.4 nM). Some SAR generalizations are discussed.

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Year:  1998        PMID： 9622557     DOI： 10.1021/jm980088f

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  3 in total

1.  Antimalarial activity of synthetic 1,2,4-trioxanes and cyclic peroxy ketals, a quantum similarity study.

Authors:  X Gironés; A Gallegos; R Carbó-Dorca
Journal:  J Comput Aided Mol Des       Date:  2001-12       Impact factor: 3.686

2.  Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.

Authors:  Andrew S Rosenthal; Xiaochun Chen; Jun O Liu; Diana C West; Paul J Hergenrother; Theresa A Shapiro; Gary H Posner
Journal:  J Med Chem       Date:  2009-02-26       Impact factor: 7.446

3.  Artemisinin and a series of novel endoperoxide antimalarials exert early effects on digestive vacuole morphology.

Authors:  Maria del Pilar Crespo; Thomas D Avery; Eric Hanssen; Emma Fox; Tony V Robinson; Peter Valente; Dennis K Taylor; Leann Tilley
Journal:  Antimicrob Agents Chemother       Date:  2007-10-15       Impact factor: 5.191
  3 in total

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