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Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum.
| Publication Type | Journal Article |
| Authors | Martyn, DC, Ramirez AP, Beattie MJ, Cortese JF, Patel V., Rush MA, Woerpel KA, and Clardy J. |
| Abstract | Artemisinin-derived compounds play an integral role in current malaria chemotherapy. Given the virtual certainty of emerging resistance, we have investigated spiro-1,2-dioxolanes as an alternative scaffold. The endoperoxide functionality was generated by the SnCl(4)-mediated annulation of a bis-silylperoxide and an alkene. The first set of eight analogs gave EC(50) values of 50-150 nM against Plasmodium falciparum 3D7 and Dd2 strains, except for the carboxylic acid analog. A second series, synthesized by coupling a spiro-1,2-dioxolane carboxylic acid to four separate amines, afforded the most potent compound (EC(50) approximately 5 nM). |
| Year of Publication | 2008 |
| Journal | Bioorganic & medicinal chemistry letters |
| Volume | 18 |
| Issue | 24 |
| Pages | 6521-4 |
| Date Published (YYYY/MM/DD) | 2008/12/15 |
| ISSN Number | 0960-894X |
| DOI | 10.1016/j.bmcl.2008.10.083 |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/18993067?dopt=Abstract |
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