| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1367640 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
The antimalarial activity of chloroquine-pyrazole analogues, synthesized from the reaction of 1,1,1-trifluoro-4-methoxy-3-alken-2-ones with 4-hydrazino-7-chloroquinoline, has been evaluated in vitro against a chloroquine resistant Plasmodium falciparum clone. Parasite growth in the presence of the test drugs was measured by incorporation of [3H]hypoxanthine in comparison to controls with no drugs. All but one of the eight (4,5-dihydropyrazol-1-yl) chloroquine 2 derivatives tested showed a significant activity in vitro, thus, are a promising new class of antimalarials. The three most active ones were also tested in vivo against Plasmodium berghei in mice. However, the (pyrazol-1-yl) chloroquine 3 derivatives were mostly inactive, suggesting that the aromatic functionality of the pyrazole ring was critical.
Graphical abstractThe antimalarial activity of 4,5-dihydropyrazole and pyrazole chloroquine analogues is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
