Journal Article
| Title | Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates. |
| Publication Type | Journal Article |
| Authors | Araújo, NCP, Barton, V, Jones, M, Stocks, PA, Ward, SA, Davies, J, Bray, PG, Shone, AE, Cristiano, MLS, O'Neill, PM |
| Year of Publication | 2009 |
| Journal | Bioorg Med Chem Lett |
| Volume | 19 |
| Issue | 7 |
| Date Published | 2009 Apr 1 |
| Pagination | 2038-43 |
| ISSN | 1464-3405 |
| Keywords | Aminacrine, Animals, Antimalarials, Artemisinins, Peroxides, Plasmodium falciparum, Quinolines, Structure-Activity Relationship |
| Abstract | A novel series of semi-synthetic trioxaquines and synthetic trioxolaquines were prepared, in moderate to good yields. Antimalarial activity was evaluated against both the chloroquine-sensitive 3D7 and resistant K1 strain of Plasmodium falciparum and both series of compounds were shown to be active in the low nanomolar range. For comparison the corresponding 9-amino acridine analogues were also prepared and shown to have low nanomolar activity like their quinoline counterparts. |
| DOI | 10.1016/j.bmcl.2009.02.013 |
| Sapientia | |
| Alternate Journal | Bioorg. Med. Chem. Lett. |
| PubMed ID | 19251414 |
| Grant List | BB/C006321/1 / / Biotechnology and Biological Sciences Research Council / United Kingdom BBS/B/05508 / / Biotechnology and Biological Sciences Research Council / United Kingdom BBS/Q/Q/2004/06032 / / Biotechnology and Biological Sciences Research Council / United Kingdom BBS/S/P/2003/10353 / / Biotechnology and Biological Sciences Research Council / United Kingdom |
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